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1
EPR characterization of mono(thiosemicarbazones) copper(II) complexes. Note II.
2000-04-01

Copper(II) complexes with thiosemicarbazones have been shown to be more active in cell destruction, in the inhibition of DNA synthesis than the uncomplexed ligand. Several derivatives of thiosemicarbazones and their iron and copper complexes have been studied for their cytotoxicity and inhibiting activity against DNA ...

PubMed

2
Synthesis and spectral characterization of acetophenone thiosemicarbazone--a nonlinear optical material.
2010-03-23

Acetophenone thiosemicarbazone (APTSC) was synthesized. Solubility of APTSC was determined in ethanol and methanol at different temperatures. Single crystals were grown from ethanol by slow evaporation at room temperature. The grown crystal was subjected to FTIR, Laser-Raman and (1)H NMR spectral analyses to confirm the synthesized compound. Thermal ...

PubMed

3
Synthesis, spectral characterization and eukaryotic DNA degradation of thiosemicarbazones and their platinum(IV) complexes.
2007-03-16

The condensation products of acetophenone (or its derivatives), salicylaldehyde and o-hydroxy-p-methoxybenzophenone with thiosemicarbazide and ethyl- or phenyl-thiosemicarbazide are the investigated thiosemicarbazones. Their reactions with H(2)PtCl(6) produced Pt(IV) complexes characterized by elemental, thermal, mass, IR and electronic spectral studies. ...

PubMed

4
Synthesis and screening of substituted thiosemicarbazone derivatives: an approach towards novel anticonvulsant search.
2011-03-01

A series of thiosemicarbazones of halogen substituted benzaldehydes, benzophenone and acetophenone were synthesized using an appropriate synthetic route and characterized by thin layer chromatography and spectral analysis. The anticonvulsant activity of synthesized compounds was established in three seizures models which includes maximal electroshock ...

PubMed

5
Methyl substituent at C(2) carbon of acetophenone thiosemicarbazone induces unusual heterobridging in the [(Ph(3)P)Cu(mu-I)(2)(mu-S-Haptsc)Cu(PPh(3))] dimer.
2007-06-29

The sulfur of acetophenone thiosemicarbazone {(Ph)(Me)C=N-NH-C(=S)NH(2); Haptsc} and two iodine atoms form an unusual heterobridge in the dinuclear complex [(Ph(3)P)Cu(mu-I)(2)(mu-S-Haptsc)Cu(PPh(3))] (1), leading to a short Cu--Cu distance of 2.504(1) Angstrom. This uncommon heterobridging is attributed to the presence of a methyl substituent at the ...

PubMed

6
Preferential Inhibition of Ribonucleic Acid Synthesis by a New ...

... Title : Preferential Inhibition of Ribonucleic Acid Synthesis by a New Thiosemicarbazone Possessing Antibacterial and Antiparasitic Properties. ...

DTIC Science & Technology

7
Preferential inhibition of ribonucleic acid synthesis by a new thiosemicarbazone possessing antibacterial and antiparasitic properties.
1981-02-01

We determined the influence of the azacycloheptane derivative (H) of a 2-acetylpyridine thiosemicarbazone on growth and macromolecular synthesis in Escherichia coli AT-9. Thiosemicarbazone H caused bacteriostasis and a primary inhibition of ribonucleic acid synthesis; secondary effects included inhibition of ...

PubMed Central

8
Organometallic ruthenium complexes with thiosemicarbazone ligands: Synthesis, structure and cytotoxicity of [(?6-p-cymene)Ru(NS)Cl]+ (NS = 9-anthraldehyde thiosemicarbazones)
2009-11-01

A series of half-sandwich arene-ruthenium complexes of the type [(?6-p-cymene) Ru(thiosemicarbazone)Cl]+ have been synthesized and their biological activity investigated. The first structurally characterized arene-ruthenium half-sandwich complex with a thiosemicarbazone ligand is reported.

PubMed Central

9
Preferential Inhibition of Ribonucleic Acid Synthesis by a New ...
2011-05-14

... Thiosemicarbazones containing highly varied product of Nutritional Biochemicals Corp., Cleveland, substituents have been found to possess ...

DTIC Science & Technology

10
Chapter II General Overview of the Analytical Techniques

of the synthesis and characterizations of all the materials used during the thesis. This part is subdivided in two.3.1 Synthesis of Thiosemicarbazone based Ligands 2.3.1.1 Pyridoxal-4R-thiosemicarbazone hydrochloride (R = H, CH in vacuo for two days. Pyridoxal thiosemicarbazone hydrochloride ...

E-print Network

11
Chapter IV Tuning of the Charge in Octahedral Ferric

.2.1 Synthesis2 The pyridoxal-N-substituted thiosemicarbazone hydrochloride derivatives (scheme 4.1) were+ R = H, CH3, CH3CH2 Scheme 4.1. Synthesis of pyridoxal-N-substituted thiosemicarbazone monohydrate characterized examples have already been reported.22-27 Reaction of pyridoxal-N-substituted ...

E-print Network

12
Thiosemicarbazones: the new wave in cancer treatment.
2009-09-01

The anticancer effects of thiosemicarbazones were once solely attributed to the inhibition of ribonucleotide reductase, an enzyme involved in the rate-limiting step of DNA synthesis. However, the mechanism behind this inhibition was initially not described. The ability of thiosemicarbazones to chelate metal ions has now been recognized ...

PubMed

13
Synthesis of thiosemicarbazone and 4-thiazolidinone derivatives and their in vitro anti-Toxoplasma gondii activity.
2005-05-16

Thiosemicarbazone and 4-thiazolidinone derivatives were synthesized in one and two step, respectively, from thiosemicarbazide, in satisfactory yields. Then, the synthesized compounds were submitted to evaluation against host cells infected with Toxoplasma gondii. The present studies showed that thiosemicarbazones 2 and 4-thiazolidinone derivatives 3 were ...

PubMed

14
Identification and characterization of thiosemicarbazones with antifungal and antitumor effects: cellular iron chelation mediating cytotoxic activity.
2008-08-13

Thiosemicarbazones derived from acetylpyrazines were prepared by condensing an acetylpyrazine or a ring-substituted acetylpyrazine with thiosemicarbazide. Using the same procedure, N, N-dimethylthiosemicarbazones were synthesized from acetylpyrazines and N, N-dimethylthiosemicarbazide. A total of 20 compounds (16 novel) were chemically characterized and then tested for ...

PubMed

15
Isatin-?-thiosemicarbazones as potent herpes simplex virus inhibitors.
2011-02-15

A series of isatin-?-thiosemicarbazones have been designed and evaluated for antiviral activity against herpes simplex virus type 1 (HSV-1) and type 2 (HSV-2) in a plaque reduction assay. Their cytotoxicity was examined using human rhabdomyosarcoma cells (RD cells). Several derivatives of isatin-?-thiosemicarbazone exhibited significant and selective ...

PubMed

16
Functionalized benzophenone, thiophene, pyridine, and fluorene thiosemicarbazone derivatives as inhibitors of cathepsin L.
2010-09-15

A series of thiosemicarbazone analogs based on the benzophenone, thiophene, pyridine, and fluorene molecular frameworks has been prepared by chemical synthesis and evaluated as small-molecule inhibitors of the cysteine proteases cathepsin L and cathepsin B. The two most potent inhibitors of cathepsin L in this series (IC(50)<135 nM) are ...

PubMed

17
SYNTHESIS OF GEM-DISUBSTITUTED THIAZOLINES
1962-05-31

... times to removet unreacted thiourea. ... changed a brown solid-like paste.) The reaction mixture became very sticky ... (1) Acetophenone oxime. 9 0 ...

DTIC Science & Technology

18
REPORT Oq /xv -.p _-c_../L-.--"- THE SYNTHESIS OF MONOMERS WITH ...

monomers, which was not successful for the preparation of I was, h_0wever, successful with (phenylethynyi)trifluoromethyl- acetophenone. 12(Scheme ...

NASA Website

19
Nuclear medicine program: Progress report for quarter ending June 30, 1988
1989-02-01

This report describes our initial studies on developing techniques of attaching radioisotopes of copper (Cu-64 and Cu-67) and rhenium (Re-186 and Re-188) to proteins. Our work has focussed on the synthesis of para-carboxyalkylphenylglyoxal-bis-(N/sub 4/-methylthiosemi-carbazone) ligands (TSC). Because of the strong binding of Cu(II) to the bis-TSC ligand, the development of ...

Energy Citations Database

20
Synthesis of some new 4(3H)-quinazolinone-2-carboxaldehyde thiosemicarbazones and their metal complexes and a study on their anticonvulsant, analgesic, cytotoxic and antimicrobial activities - part-1.
2010-04-27

Novel 3-aryl-4(3H)-quinazolinone-2-carboxaldehydes, their corresponding Schiff's base and thiosemicarbazone derivatives were synthesized from the starting 5-iodo anthranilic acid. Copper(II), zinc(II) complexes of some thiosemicarbazone derivatives were also synthesized and characterized. Screening for some selected compounds was carried out to probe their ...

PubMed

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21
Synthesis and antitumor activity of liquiritigenin thiosemicarbazone derivatives.
2010-05-06

In an attempt to develop potent and selective antitumor agents, a series of liquiritigenin thiosemicarbazone derivatives were designed and synthesized. The cytotoxicities of these compounds were evaluated in vitro against K562, DU-145, SGC-7901, HCT-116 and Hela cell lines. The pharmacological results showed that most of the prepared compounds displayed excellent selective ...

PubMed

22
Nickel (II) complexes of naphthaquinone thiosemicarbazone and semicarbazone: synthesis, structure, spectroscopy, and biological activity.
2005-07-01

Ni(II) complexes of ortho-naphthaquinone thiosemicarbazone and semicarbazone were synthesized and spectroscopically characterized. The X-ray crystal structure of both the complexes describe a distorted octahedral coordination with two tridentate mono-deprotonated ligands. In vitro anticancer studies on MCF-7 human breast cancer cells reveal that the semicarbazone derivative ...

PubMed

23
Total synthesis of norneolignans from Krameria species.
2004-12-01

The total synthesis of nomeolignans isolated from Krameria species, 2-aryl-5-(E)-propenylbenzofurans (5, 11), is described. The key step involves the one-pot reaction for 2-arylbenzofurans (2, 7) from 4-hydroxyphenylacetone with 4'-acetoxy-2-chloro-2-(methylthio)acetophenone (1) and ...

PubMed

24
Facile, High Yield Synthesis of 2,3-Diphenyl-1,3-Butadiene.
1986-01-01

A high yield. four step synthesis process is disclosed for producing the monomer, 2,3-diphenyl-1,3-butadiene, wherein in step 1 acetophone pinacol is produced from the dimerization of acetophenone in 96% yield; in step 2 acetophenone pinacol is reacted wi...

National Technical Information Service (NTIS)

25
Polish Pharmaceutical Transactions, Vol. 24, No. 2, 1967.
1967-01-01

Contents: Studies on reactions of thiosemicarbazones with haloketones. Part V; Nicotinic acid derivatives. II. Synthesis of some derivatives of 2-amino-3-cyanopyridyne and 2-aminonicotinic acid; Studies on potential hypotensive substances. V. Synthesis of...

National Technical Information Service (NTIS)

26
Microwave synthesis of mixed ligand diimine�thiosemicarbazone complexes of ruthenium(ii): biophysical reactivity and cytotoxicity�
2009-09-28

A novel microwave-assisted synthetic method has been used to synthesise a series of mixed ligand ruthenium(ii) compounds containing diimine as well as bidentate thiosemicarbazone ligands. The compounds contain the diimine 1,10-phenanthroline (phen) or 2,2?-bipyridine (bpy) and the thiosemicarbazone is derived from 9-anthraldehyde. Based on elemental ...

PubMed Central

27
Microwave synthesis of mixed ligand diimine-thiosemicarbazone complexes of ruthenium(II): biophysical reactivity and cytotoxicity.
2009-09-28

A novel microwave-assisted synthetic method has been used to synthesise a series of mixed ligand ruthenium(II) compounds containing diimine as well as bidentate thiosemicarbazone ligands. The compounds contain the diimine 1,10-phenanthroline (phen) or 2,2'-bipyridine (bpy) and the thiosemicarbazone is derived from 9-anthraldehyde. Based on elemental ...

PubMed

28
Synthesis, characterization, and antifungal activity of boron-containing thiosemicarbazones.
2008-11-01

Addition of thiosemicarbazide, 4-allylthiosemicarbazide, and 4-phenylthiosemicarbazide to (formylphenyl)boronic acids affords a series of thiosemicarbazones containing boronic acids. Addition of 2-formylphenylboronic acid to the thiosemicarbazides gave the corresponding cyclic 2,3,1-benzodiazaborines. All new compounds have been investigated for potential antifungal activity. ...

PubMed

29
A New Synthesis of Substituted Pyrazoles from 1,4-Dianions of Phenylhydrazones Having an Alpha-Hydrogen.
1970-01-01

The 1,4-dianions of acetophenone, para-substituted acetophenones, deoxybenzoin and dibenzyl ketone phenylhydrazone were prepared by treatment of the respective phenylhydrazone with two molecular equivalents of n-butyllithium in tetrahydrofuran-hexane at 0...

National Technical Information Service (NTIS)

30
Synthesis and structure-activity correlation studies of metal complexes of alpha-N-heterocyclic carboxaldehyde thiosemicarbazones in Shewanella oneidensis.
2005-04-01

This investigation involved the synthesis of metal complexes to test the hypothesis that structural changesand metal coordination in pyridine thiosemicarbazones affect cell growth and cell proliferation in vitro. Thiosemicarbazones are well known to possess antitumor, antiviral, antibacterial, antimalarial, and other activities. ...

PubMed

32
Synthesis, cytotoxic and antimalarial activities of benzoyl thiosemicarbazone analogs of isoquinoline and related compounds.
2010-02-23

Thiosemicarbazone analogs of papaveraldine and related compounds 1-6 were synthesized and evaluated for cytotoxic and antimalarial activities. The cytotoxic activity was tested against HuCCA-1, HepG2, A549 and MOLT-3 human cancer cell lines. Thiosemicarbazones 1-5 displayed cytotoxicity toward all the tested cell lines, while compounds 2-5 selectively ...

PubMed

33
Synthesis of Multifunction Triaryltrifluoroethanes.
1978-01-01

New 1,1,1-triaryl 2,2,2-trifluoro ethanes in which the aryl radicals carry one or more substituents, were prepared by condensing trifluoro acetophenones with substituted aromatic compounds in the presence of catalytic quantities of trifluoro methyl sulfon...

National Technical Information Service (NTIS)

34
SYNTHESIS OF 1-PHENYLPROPYNE-2, 3-13C21,
1964-04-09

... Abstract : A method of preparing the title compound from methyl-13C iodide through acetophenone-2-13C, 1-phenylethanol-2-13C, styrene-2-13C ...

DTIC Science & Technology

35
Polyanthrazolines.
1972-01-01

The basic condensation of acetophenone with benzo (1,2-b; 5,4-b') - dipyrrolo-2,3,5,6-tetraone gives the substituted anthrazoline compound in good yield. Since this reaction type appeared to be an excellent route for the synthesis of some thermally stable...

National Technical Information Service (NTIS)

36
An efficient one-pot synthesis of 2,3-epoxyl-1,3-diaryl-1-propanone directly from acetophenones and aromatic aldehydes under ultrasound irradiation.
2009-09-26

A convenient and efficient one-pot synthesis of 2,3-epoxyl-1,3-diaryl-1-propanone directly from acetophenones and aromatic aldehydes under ultrasound irradiation at room temperature has been described. In comparison to two-step methods, the present procedure has the advantages of mild conditions, shorter reaction time, without isolation of any ...

PubMed

37
synthesis, characterization and in vitro antiamoebic activity of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones and their Palladium (II) and Ruthenium (II) complexes.
2004-05-01

Synthesis of new Palladium(II) and Ruthenium(II) complexes of the type, [Pd(L)Cl(2)] and [Ru(eta(4)-C(8)H(12))(L)Cl(2)] [where, L = thiosemicarbazones derived from 5-nitrothiophene-2-carboxaldehyde and cycloalkylaminothiocarbonyl hydrazines] have been isolated by the reaction of [Pd(DMSO)(2)Cl(2)] and [Ru(eta(4)-C(8)H(12))(CH(3)CN)(2)Cl(2)] with ...

PubMed

38
Synthesis, spectroscopic and physicochemical characterization and biological activity of Co(II) and Ni(II) coordination compounds with 4-aminoantipyrine thiosemicarbazone.
2005-01-01

We describe the synthesis and characterization of cobalt(II) and nickel(II) coordination compounds of 4[N-(furan-2'-aldimine)amino]antipyrine thiosemicarbazone (FFAAPTS) and 4[N-(4'-nitrobenzalidene) amino]antipyrine thiosemicarbazone (4'-NO(2)BAAPTS). All the isolated compounds have the general composition MX(2)(L)(H(2)O) (M = Co(2+) ...

PubMed

39
Synthesis and spectroscopic properties of copper(II) complexes derived from thiophene-2-carbaldehyde thiosemicarbazone. Structure and biological activity of [Cu(C6H6N3S2)2].
1999-05-30

The synthesis, structure and spectroscopic properties on complexes with the formula [Cu(Lm)2] (1) and Cu(NO3)2(HLm)2 (2), where HLm = thiophene-2-carbaldehyde thiosemicarbazone, have been developed. The molecular structure of compound 1 consists of monomeric entities. The copper(II) ions exhibit distorted square-planar geometry with both bidentate ...

PubMed

40
Synthesis and in vitro evaluation of gold(I) thiosemicarbazone complexes for antimalarial activity.
2010-07-01

The reaction of thiosemicarbazones (TSCs) with [Au(I)(THT)Cl], THT=tetrahydrothiophene, has been investigated. The resulting gold(I) complexes have been characterized by a range of spectroscopic techniques: NMR spectroscopy, mass spectrometry, microanalysis and infrared spectroscopy. The in vitro antimalarial data for gold(I) TSC complexes suggests that coordination of gold(I) ...

PubMed

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41
Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB
2008-04-08

Human African trypanosomiasis (HAT) is caused by the protozoan parasite Trypanosoma brucei. The cysteine proteases of T.brucei have been shown to be crucial for parasite replication and represent an attractive point for therapeutic intervention. Herein we describe the synthesis of a series of thiosemicarbazones and their activity against the trypanosomal ...

PubMed Central

42
Preparing Students for Research: Synthesis of Substituted Chalcones as a Comprehensive Guided-Inquiry Experience
2002-09-01

A guided inquiry experiment involving the synthesis and characterization of substituted benzalacetophenones (chalcones) is described. The chalcones are produced in the aldol condensation of substituted benzaldehydes with substituted acetophenones. Each student is assigned a different target chalcone and conducts online and printed literature searches on ...

NASA Astrophysics Data System (ADS)

43
Chemoenzymatic asymmetric total synthesis of (S)-Rivastigmine using omega-transaminases.
2010-05-11

A straightforward, high-yielding, chemoenzymatic total synthesis of enantiopure (S)-Rivastigmine was developed using various omega-transaminases for the asymmetric amination of appropriate acetophenone precursors. Optimisation of the biotransformation allowed scale-up and the total synthesis of (S)-Rivastigmine. PMID:20461261

PubMed

44
Synthesis and insecticidal activities of novel oxime ether pyrethroids.
2005-02-01

A series of novel 2-methylthio-3'/4'-substituted acetophenone oxime O-ethers were synthesized by the reaction of the corresponding acetophenone oximes with halides of pyrethroid alcohols in the presence of sodium hydroxide and phase-transfer catalysis or with triethyl quaternary ammonium salts of halides of pyrethroid alcohols in the presence of sodium ...

PubMed

45
Synthesis, structural characterization and biological activity of p-fluorobenzaldehyde thiosemicarbazones and of a nickel complex.
2000-07-15

New thiosemicarbazones (1-7), derived from p-fluorobenzaldehyde and differently substituted thiosemicarbazides, were synthetized and characterized by means of NMR and IR techniques. The p-fluorobenzaldehyde thiosemicarbazone Hfbt (1), the p-fluorobenzaldehyde 4-phenylthiosemicarbazone Ph-Hfbt (4) and complex [Ni(fbt)2] (8) were also characterized by X-ray ...

PubMed

46
Synthesis, characterization and antiamoebic activity of new indole-3-carboxaldehyde thiosemicarbazones and their Pd(II) complexes.
2007-03-02

In continuation of our research on thiosemicarbazones and their metal complexes as antiamoebic agents, a new series of indole-3-carboxaldehyde thiosemicarbazones (TSC) 1-7 were prepared by condensing indole-3-carboxaldehyde with cycloalkylaminothiocarbonyl hydrazines. Their palladium(II) complexes of the [Pd(TSC)Cl2] type, were synthesized upon ...

PubMed

47
Synthesis, activity and pharmacophore development for isatin-?-thiosemicarbazones with selective activity towards multidrug resistant cellsa
2009-05-28

We have recently identified a new class of compounds that selectively kill cells that express P-glycoprotein (P-gp, MDR1), the ATPase efflux pump that confers multidrug resistance on cancer cells. Several isatin-?-thiosemicarbazones from our initial study have been validated, and a range of analogs synthesized and tested. A number demonstrated improved MDR1-selective activity ...

PubMed Central

48
Synthesis and antimalarial activity of semicarbazone and thiosemicarbazone derivatives.
2007-11-26

Seventeen semicarbazone and thiosemicarbazone derivatives were prepared and tested in vitro against a chloroquine resistant strain of Plasmodium falciparum (W2) to evaluate their antiplasmodial potential. Three thiosemicarbazones were found to be active against the parasite and non-toxic to human peripheral blood mononuclear cells (PBMC). Among these, ...

PubMed

49
Synthesis, spectroscopic characterization and biological properties of new natural aldehydes thiosemicarbazones.
2000-01-01

As part of a research programme aimed at the synthesis of compounds with antiviral, antibacterial and antitumor properties and their spectroscopic characterization, new thiosemicarbazones deriving from natural aldehydes have been investigated. These substances contain in the same molecule both a chain with nucleophilic centres N, S with tubercolostatic ...

PubMed

50
Design, synthesis, and biochemical evaluation of novel cruzain inhibitors with potential application in the treatment of Chagas' disease.
2006-06-15

A series of compounds bearing tetrahydronaphthalene, benzophenone, propiophenone, and related rigid molecular skeletons functionalized with thiosemicarbazone or unsaturated carbonyl moieties were prepared by chemical synthesis and evaluated for their ability to inhibit the enzyme cruzain. As potential treatment agents for Chagas' disease, three compounds ...

PubMed

51
Necessary and sufficient conditions for the asymmetric synthesis of chiral amines using ?-aminotransferases.
2011-02-01

The half reactions of ?-aminotransferase (?-AT) from Vibrio fluvialis JS17 (?-ATVf) were carried out using purified pyridoxal 5'-phosphate-enzyme (PLP-Enz) and pyridoxamine 5'-phosphate-enzyme (PMP-Enz) complexes to investigate the relative activities of substrates. In the reaction generating PMP-Enz from PLP-Enz using L-alanine as an amine donor, L-alanine showed about 70% of the initial reaction ...

PubMed

52
Synthesis, Structural Characterization, and Pro-apoptotic Activity of 1-Indanone Thiosemicarbazone Platinum(II) and Palladium(II) Complexes: Potential as Antileukemic Agents.
2011-05-23

In the search for alternative chemotherapeutic strategies against leukemia, various 1-indanone thiosemicarbazones, as well as eight novel platinum(II) and palladium(II) complexes, with the formula [MCl(2) (HL)] and [M(HL)(L)]Cl, derived from two 1-indanone thiosemicarbazones were synthesized and tested for antiproliferative activity against the human ...

PubMed

53
Synthesis and anticonvulsant evaluation of some novel (thio)semicarbazone derivatives of arylalkylimidazole.
2011-01-01

A number of novel 2-(1H-imidazole-1-yl)-1-aryl-substituted ethane-1-one N-substituted phenyl(thio)semicarbazones (1-14) were synthesized to test for their anticonvulsant activity against the two seizure models, maximal electroshock (MES) and subcutaneous pentylenetetrazol (scPTZ). Title compounds were prepared by the reaction of appropriate (thio)semicarbazides with ketones. Neurotoxicity was ...

PubMed

54
Cyclooctadiene Ru(II) complexes of thiophene-2-carboxaldehyde-derived thiosemicarbazones: synthesis, characterization and antiamoebic activity.
2006-03-20

Thiosemicarbazones (TSC) 1-10 were synthesized by condensing substituted thiosemicarbazide with thiophene-2-carboxaldehyde. These thiosemicarbazones were further reacted with [Ru(eta4-C8H12)(CH3CN)2Cl2] to form complexes of the type [Ru(eta4-C8H12)(TSC)Cl2] 1a-10a. Thiosemicarbazones exhibited antiamoebic activity in the range ...

PubMed

55
Synthesis of parvistemin A via biomimetic oxidative dimerization.
2011-06-06

The first synthesis of the naturally occurring benzoquinone dimer parvistemin A is reported. The key step is the late stage iron(III) mediated dimerization of a 1,2,4-trihydroxyarene to give the natural product in good yield, a phenol oxidative coupling that is believed to be biomimetic. The route proceeds in seven steps from an inexpensive commercially available ...

PubMed

56
Nobiletin metabolites: Synthesis and inhibitory activity against matrix metalloproteinase-9 production.
2011-06-12

A divergent synthesis of nobiletin metabolites was developed through highly oxygenated acetophenone derivative. We used commercially available methyl 3,4,5-trimethoxybenzoate as a starting material for concise preparation of the key intermediate, 2'-hydroxy-3',4',5',6'-tetramethoxyacetophenone (I). These metabolites showed strong inhibitory activity ...

PubMed

57
Chemiexcitation of Acetophenone via the Non-Adiabatic Thermal Rearrangement of Dewar Acetophenone.
1974-01-01

A study of the thermolysis of Dewar acetophenone to acetophenone is reported. This valence isomerization is found to proceed to a small degree (approx. 0.1%) via the non-adiabatic chemiexcitation of triplet acetophenone. Comparison of the activation param...

National Technical Information Service (NTIS)

58
Synthesis, spectral studies and in vitro assessment for antiamoebic activity of new cyclooctadiene ruthenium(II) complexes with 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones.
2005-10-06

We report here the synthesis, characterization and in vitro antiamoebic activity of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazones (TSC), 1-5, and their bidentate complexes [Ru(eta(4)-C(8)H(12))(TSC)Cl(2)] 1a-5a. The biological studies of these compounds were investigated against HK-9 strain of Entamoeba histolytica and the concentration causing 50% ...

PubMed

59
Synthesis and characterization of Pd(II) and Pt(II) complexes of p-isopropylbenzaldehyde N-protected thiosemicarbazones. Cytotoxic activity against ras-transformed cells.
1999-07-15

Cytotoxicity tests in tumor cells sensitive to cis-DDP (HL-60, JURKAT, Hela and 3T3) and in tumor cells transformed by ras oncogenes and resistant to cis-DDP (Pam 212-ras) show that cyclometallated complexes 1a [Pd(p-is.TSCN-NHMe)]4, 2b [Pt(p-is.TSCN-NMe2)]4 and 4a [Pd(p-is.TSCN-NHex)]4 may be endowed with specific cytotoxic properties. In fact, these three novel ...

PubMed

60
Synthesis and characterization of tin(II) complexes of fluorinated Schiff bases derived from amino acids.
2010-03-23

New tin(II) complexes of general formula Sn(L)(2) (L=monoanion of 3-methyl-4-fluoro-acetophenone phenylalanine L(1)H, 3-methyl-4-fluoro-acetophenone alanine L(2)H, 3-methyl-4-fluoro acetophenone tryptophan L(3)H, 3-methyl-4-fluoro-acetophenone valine L(4)H, 3-methyl-4-fluoro-acetophenone ...

PubMed

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61
Solvothermal synthesis and characterisation of La{sub 1-} {sub x}A{sub x} MnO{sub 3} nanoparticles
2006-10-15

The synthesis of La{sub 1-} {sub x}A{sub x} 3 (A=Ca, Sr, Ba) nanoparticles in nonaqueous solvents has been studied. For this solvothermal procedure benzyl alcohol and acetophenone were chosen as reaction media. After this treatment in mild conditions a precipitate was obtained, which, however, can be annealed to the crystalline perovskite structure. Our ...

Energy Citations Database

62
Microwave assisted tandem reactions for the synthesis of 2-hydrazolyl-4-thiazolidinones
2009-02-25

A tandem method for the synthesis of 2-hydrazolyl-4-thiazolidinones (5) from commercially available materials in a 3 component reaction has been developed. The reaction connects aldehydes, thiosemicarbazides and maleic anhydride, effectively assisted by microwave irradiation. The synthesis of a new type of compound, ...

PubMed Central

63
Cellular confocal fluorescence studies and cytotoxic activity of new Zn(II) bis(thiosemicarbazonato) complexes.
2008-03-18

We report the synthesis and characterisation of new, highly fluorescent, zinc complexes of bis(thiosemicarbazone) ligands incorporating extended aromatic backbones which are cytotoxic at levels comparable to cisplatin; cellular fluorescence imaging studies suggest these cause cell death by disruption of mitochondria. PMID:18398535

PubMed

64
Synthesis, spectroscopic and toxicity studies of titanocene chelates of isatin-3-thiosemicarbazones.
2005-01-01

The reactions of bis(cyclopentadienyl)titanium(IV) dichloride with a new class of thiosemicarbazone (LH(2)), derived by condensing isatin with different N(4)-substituted thiosemicarbazides, have been studied and products of type [Cp(2)Ti(L)] have been isolated. On the basis of various physico-chemical and spectral studies, five coordinate structures have been assigned to these ...

PubMed

65
Synthesis, characterisation and biological activity of three copper (II) complexes with a modified nitrogenous base: 5-formyluracil thiosemicarbazone.
1998-05-01

Three Cu(II) co-ordination compounds with a novel ligand, 5-formyluracil thiosemicarbazone (H3ut), have been synthesised and characterised by single-crystal X-ray diffraction and subsequently tested in vitro on human leukemic cells. The crystal structures revealed, in all three cases, a square pyramidal co-ordination geometry of the copper atom with the ligand lying on the ...

PubMed

66
Synthesis, antimicrobial and anticancer activity of new thiosemicarbazone derivatives.
2010-11-25

Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, ...

PubMed

67
Synthesis, Spectroscopic and Toxicity Studies of Titanocene Chelates of Isatin-3-Thiosemicarbazones
2005-01-01

The reactions of bis(cyclopentadienyl)titanium(IV) dichloride with a new class of thiosemicarbazone (LH2), derived by condensing isatin with different N(4)-substituted thiosemicarbazides, have been studied and products of type [Cp2Ti(L)] have been isolated. On the basis of various physico-chemical and spectral studies, five ...

PubMed Central

68
Synthesis, Antimicrobial and Anticancer Activity of New Thiosemicarbazone Derivatives.
2010-11-25

Thiosemicarbazones of p-aminobenzoic acid (PABA) were synthesized and tested for their antimicrobial and anticancer activity. Hydroxamate derivatives 4a-4l were found to have better antimicrobial and anticancer activity than their acid counterpart. Compound 4d was found to have good antimicrobial activity against Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, ...

PubMed

69
Synthesis and evaluation of anti-HIV activity of isatin beta-thiosemicarbazone derivatives.
2005-10-15

On the basis of pharmacophoric modelling studies of existing NNRTIs, a series of isatin beta-thiosemicarbazone derivatives was synthesized and evaluated for their anti-HIV activity in HTLV-III(B) strain in the CEM cell line. Three compounds showed significant anti-HIV activity, whereupon compound 6 was found to be the most active compound with an EC(50) value of 2.62 microM ...

PubMed

70
Synthesis and characterization of new trimeric rhenium(I) complexes. The influence of steric factors on the size of pyrazolonaterhenium(I) metallomacrocycles.
2006-09-01

The reaction of [ReX(CO)5] with thiosemicarbazones H2L(R) derived from beta-keto esters (X = Cl, Br; R = Me, Ph) allowed the isolation of cyclic trimeric complexes [Re3(pyz(R))3(CO)9], where pyz(R) is the pyrazolonate corresponding to the thiosemicarbazone. Electron spray ionization Fourier transform ion cyclotron resonance mass spectrometry (ESI-FTICR-MS) ...

PubMed

71
Synthesis and characterization of new aromatic aldehyde/ketone 4-(beta-D-glucopyranosyl)thiosemicarbazones.
2009-05-22

A series of 22 aromatic aldehyde/ketone 4-(beta-D-glucopyranosyl)thiosemicarbazones have been synthesized by condensation of 4-(per-O-acetylated-beta-D-glucopyranosyl)thiosemicarbazide with an aldehyde or a ketone, and then, deacetylation of the resulting product. The compounds were fully characterized by spectroscopic techniques, elemental analysis, and for two derivatives by ...

PubMed

72
Synthesis and Structure-Activity Evaluation of Isatin-?-thiosemicarbazones with Improved Selective Activity toward Multidrug-Resistant Cells Expressing P-Glycoprotein.
2011-08-01

Cancer multidrug resistance (MDR) mediated by ATP-binding cassette (ABC) transporters presents a significant unresolved clinical challenge. One strategy to resolve MDR is to develop compounds that selectively kill cells overexpressing the efflux transporter P-glycoprotein (MDR1, P-gp, ABCB1). We have previously reported structure-activity studies based around the lead compound NSC73306 (1, ...

PubMed

73
Synthesis, structural characterization, and biological evaluation of oxorhenium(V) complexes with a novel type of thiosemicarbazones derived from N-[N',N'-dialkylamino(thiocarbonyl)]benzimidoyl chlorides.
2009-10-01

Reactions of N-[N',N'-diethylamino(thiocarbonyl)]benzimidoyl chloride with 4,4-dialkylthiosemicarbazides give a novel class of thiosemicarbazides/thiosemicarbazones, H(2)L, which causes a remarkable reduction of cell growth in in vitro experiments. These strong antiproliferative effects are also observed for oxorhenium(V) complexes of the general composition [ReOCl(L)], which ...

PubMed

74
Synthesis, crystal structure, characterization of zinc(II), cadmium(II) complexes with 3-thiophene aldehyde thiosemicarbazone (3TTSCH). Biological activities of 3TTSCH and its complexes.
2009-12-03

The reaction of zinc(II) chloride, cadmium(II) chloride and bromide with 3-thiophene aldehyde thiosemicarbazone leads to the formation of a series of new complexes. They have been characterized by spectroscopic studies: infrared, (1)H NMR, and electronic spectra. The crystal structures of the compound [ZnCl(2)(3TTSCH)(2)] and [CdBr(2)(3TTSCH)(2)] have been determined by X-ray ...

PubMed

75
Synthesis, characterization and in vitro anti-amoebic activity of new palladium(II) complexes with 5-nitrothiophene-2-carboxaldehyde N(4)-substituted thiosemicarbazones.
2004-09-01

Reaction between [Pd(DMSO)(2)Cl(2)] (DMSO=dimethylsulfoxide) and N(4)-substituted thiosemicarbazones derived from 5-nitrothiophene-2-carboxaldehyde (L) afforded the complexes [Pd(L)Cl(2)]. These new complexes have been characterized by elemental analyses and spectroscopic studies. Spectroscopic studies reveal that thionic sulfur and azomethine nitrogen atom of ...

PubMed

76
Synthesis, X-ray crystal structures, thermal and electrochemical properties of thiosemicarbazidatodioxouranium(VI) complexes.
2010-10-04

The stable uranyl complexes, [UO(2)(L)C(9)H(19)OH], were obtained from 3,5-dichlorosalicyl-(L(I)) and salicyl-aldehyde-S-propyl-thiosemicarbazones (L(II)) with substituted-salicylaldehyde in nonyl alcohol. The structures of the complexes have been characterized by elemental analysis, IR, (1)H NMR, conductivity, magnetic moment measurements, cyclic voltammetry, thermal ...

PubMed

77
Mn(II), Co(II) and Zn(II) complexes with heterocyclic substituted thiosemicarbazones: synthesis, characterization, X-ray crystal structures and antitumor comparison.
2010-04-14

Transition metal complexes Mn(L(1))(2) (1), Mn(L(2))(2) (2), Co(L(3))(2)Cl 4H(2)O (3), Zn(L(3))(2) DMF (4), Co(HL(4))(2)(ClO(4))(2) 3H(2)O (5) and Zn(L(5))(2) DMF (6) where HL(1)=2-acetylpyridine thiosemicarbazone, HL(2)=2-acetylpyridine N(4)-methylthiosemicarbazone, HL(3)=2-benzoylpyridine thiosemicarbazone, HL(4)=2-benzoylpyridine ...

PubMed

78
Total synthesis of munchiwarin, a triprenylated chalcone from Crotalaria medicagenia.
2007-11-22

An efficient method is developed for the synthesis of the modified triprenylated chalcone, munchiwarin (1), isolated from the roots of Crotalaria medicagenia. The synthesis of 1 utilizes a Claisen-Schmidt condensation between 2,4-dihydroxy-3,5-C-diprenyl acetophenone and 4-methoxy benzaldehyde in the presence of Ba(OH)2 to yield the ...

PubMed

79
ON THIOSEMICARBAZONE-COPPER (I) COMPLEXES. PART ...
1963-08-08

... Title : ON THIOSEMICARBAZONE-COPPER (I) COMPLEXES. ... STRUCTURE, COPPER COMPOUNDS, COMPLEX COMPOUNDS ...

DTIC Science & Technology

80
Synthesis and study of certain phenylacetothioamides as lubricant additives
1981-01-01

A number of phenylacetothioamides were synthesized by the interaction of acetophenone with sulphur and amines. Phenylacetothioamides are satisfactory anti-corrosive additives of DS-II oil, amides with a phenyl radical having higher anti-corrosive properties than amides with alkyl and heterocyclic radicals. Phenylacetothioamides improve anti-wear properties of TB-20 oil. In ...

Energy Citations Database

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81
Synthesis and characterization of novel unnatural bichalcones.
2010-12-30

Five bichalcones (5-1 ~ 5-4, 9) were prepared by the reaction of biphenyl-4,4'-dicarbaldehyde (4) and 4,4'-dioxybenzaldehyde (8) with the respective acetophenone analogs via Claisen-Schmidt condensation and were then fully identified by 1H-NMR, (13)C-NMR and mass analyses. PMID:21191755

PubMed

82
SYNTHESIS OF DEUTERATED COMPOUNDS OF BIOLOGICAL INTEREST
1958-08-11

S>During an investigation on the possible differences of biological activity between normal organic compounds and their deuterated analogs, pure compounds of hexadeuteratsd valeric acid, hexadeuterated valeramide, pentadeuterated acetophenone, pentadeuterated 2-phenyl cinchoninic acid, alpha - BETA -aliphenyl- BETA -(pentadeuteriophenyl) ethylene, and alpha ...

Energy Citations Database

83
Enantioselectivity induced by oxazaborolidine supported on mesoporous silica or by its analog in homogeneous phase.
2010-05-18

The impact of immobilization of oxazaborolidines supported on silica via different substituents on the boron and nitrogen atoms is evaluated in the enantioselective reduction of acetophenone. The performances of the homogeneous analog oxazaborolidines and silica supported-ones are compared by varying different parameters. This article deals with the ...

PubMed

84
Synthesis and characterization of semicarbazone of p-hydroxy-3-methoxy acetophenone (SPH3MA) single crystal
2011-01-01

Single crystals of semicarbazone of p-hydroxy-3-methoxy acetophenone (SPH3MA) were grown by a slow evaporation solution growth technique at room temperature. This is the first report in the literature on the crystallization of SPH3MA. The cell parameters of the grown crystals were estimated by single crystal X-ray diffraction analysis. The various planes of reflection were ...

NASA Astrophysics Data System (ADS)

85
Beta-Keto Sulfoxides. Vi. Conversion Of omega-(Methylsulfinyl)Acetophenone into Di- and Tri-omega-(Methylmercapto)Acetophenone. Synthesis of alpha-Hydroxy Aldehydes, alpha-Keto Thio Esters, alpha-Keto Esters, alpha-Hydroxy Thio Esters, and alpha-Hydroxy Esters. The Chemistry of alpha-Keto Mercaptals.
1968-01-01

A convenient synthetic conversion of beta-keto sulfoxides to alpha-hydroxy aldehydes involves the sequence RCOCH2SOCH3 to RCOCH(Cl)SCH3 to RCOCH(SCH3)2 to RCH(OH)CH(SCH3)2 to RCH(OH)CHO. Convenient syntheses of mandelaldehyde, atrolactaldehyde, benzilalde...

National Technical Information Service (NTIS)

86
Synthesis, Spectroscopic and Physicochemical Characterization and Biological Activity of Co(II) and Ni(II) Coordination Compounds with 4-Aminoantipyrine Thiosemicarbazone
2005-01-01

We describe the synthesis and characterization of cobalt(II) and nickel(II) coordination compounds of 4[N-(furan-2�-aldimine)amino]antipyrine thiosemicarbazone (FFAAPTS) and 4[N-(4'-nitrobenzalidene) amino]antipyrine thiosemicarbazone (4'-NO2BAAPTS). All the isolated compounds have the general composition ...

PubMed Central

87
General Disclaimer One or more of the Following Statements may ...

obtained from acetophenone and acetylene in a nitric environ- .... tion of acetophenone for several days at room temperature, there ...

NASA Website

88
Bromohydroxy-acetophenone (BHAP): Reregistration ...
1999-03-18

... Agency (7508W) Reregistration Eligibility Decision (RED) Bromohydroxy- acetophenone (BHAP) Page 2. BHAP Page 3. ...

EPA Pesticide Factsheets

89
Total synthesis of a norneolignan from Ratanhia radix.
2002-12-01

The total synthesis of a norneolignan isolated from Ratanhia, 5-(3-hydroxypropyl)-2-(2-methoxy-4'-hydroxyphenyl)benzofuran (8), is described. The key steps contain the one-pot reaction for a 2-arylbenzofuran 6 from methyl 3-(4-hydroxyphenyl)propionate with 2-chloro-2-methylthio-(2'-methoxy-4'-acetoxy)acetophenone (5) in the presence of ZnCl2, and reductive ...

PubMed

90
Synthesis, characterization and biological activity of two new polymeric copper(II) complexes with alpha-ketoglutaric acid thiosemicarbazone.
2002-04-10

In this paper we describe the synthesis of new copper complexes with alpha-ketoglutaric acid thiosemicarbazone. The crystal structures of the two compounds: [Cu(H(2)ct)Cl](n) [(Cu(H(2)ct)Cl)(2)] (1) and [Cu(Hct)](n).3nH(2)O (2) (H(3)ct=alpha-ketoglutaric acid thiosemicarbazone) have been determined by X-ray and spectroscopic methods. ...

PubMed

91
Microscale Synthesis of Chiral Alcohols via Asymmetric Catalytic Transfer Hydrogenation
2009-01-01

Synthesis of pure enantiomers is a key issue in industry, especially in areas connected to life sciences. Catalytic asymmetric synthesis has emerged as a powerful and practical tool. Here we describe an experiment on racemic reduction and asymmetric reduction via a catalytic hydrogen transfer process. Acetophenone and substituted ...

ERIC Educational Resources Information Center

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