Journal ArticleDOI
Synthesis, Biological Evaluation, and Quantitative Structure−Activity Relationship Analysis of New Schiff Bases of Hydroxysemicarbazide as Potential Antitumor Agents†
Shijun Ren,Rubin Wang,Kenichi Komatsu,Patricia Bonaz-Krause,Yegor Zyrianov,Charles E. McKenna,Csaba Csipke,Zoltán A. Tökés,Eric J. Lien +8 more
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TLDR
Quantitative structure-activity relationship (QSAR) analysis showed that, besides the essential pharmacophore (-NHCONHOH), hydrophobicity, molecular size/polarizability, and the presence of an oxygen-containing group at the ortho position (I) were important determinants for the antitumor activities.Abstract:
Thirty Schiff bases of hydroxysemicarbazide (Ar−CHNNHCONHOH) have been synthesized and tested against L1210 murine leukemia cells. The IC50 values were found to be in a range from 2.7 × 10-6 to 9.4 × 10-4 M. A total of 17 out of the 30 compounds had higher inhibitory activities than hydroxyurea (an anticancer drug currently used for the treatment of melanoma, leukemia, and ovarian cancer) against L1210 cells. Six compounds with IC50 values in micromolar range were 11- to 30-fold more potent than hydroxyurea (IC50 = 8.2 × 10-5 M). The partition coefficient (log P) and ionization constants (pKa) of a model compound [1-(3-trifluoromethylbenzylidene)-4-hydroxysemicarbazide, 1] were measured by the shake-flask method, and the measured log P was used to derive Hansch−Fujita π constant of −CHNNHCONHOH. On the basis of the newly derived π and those of other moieties, the partition coefficients (SlogP) of the other 29 compounds were calculated by the summation of π values. Quantitative structure−activity relations...read more
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Characterization, molecular modeling and antimicrobial activity of metal complexes of tridentate Schiff base derived from 5-acetyl-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione and 2-aminophenol.
TL;DR: The antimicrobial activities of the synthesized compounds were tested in vitro against the sensitive organisms Staphylococcus aureus as Gram positive bacteria, Proteus vulgaris as Gram negative bacteria and Candida albicans as fungus strain, and the results are discussed.
Journal ArticleDOI
Compare of three ways of synthesis of simple Schiff base
Zhaoqi Yang,Pinhua Sun +1 more
TL;DR: In this article, the synthesis of (E)-4-methyl-N-(3,4,5-trimethoxybenzylidene) benzenamine in different ways and compare of the way of synthesize it.
Journal ArticleDOI
Synthesis, spectroscopic characterization, thermal studies, catalytic epoxidation and biological activity of chromium and molybdenum hexacarbonyl bound to a novel N2O2 Schiff base
TL;DR: In this article, the antimicrobial properties of M(CO) 6 with novel Schiff base N,N′-bis(salicylidene)4,5-dichloro-1,2-phenylenediamine (H 2 L) were compared with some known antibiotics.
Journal ArticleDOI
Polymer complexes. LXXIV. Synthesis, characterization and antimicrobial activity studies of polymer complexes of some transition metals with bis-bidentate Schiff base
S.G. Nozha,Sh.M. Morgan,S. E. Abu Ahmed,M.A. El-Mogazy,M.A. Diab,Adel Z. El-Sonbati,Mohamed I. Abou-Dobara +6 more
TL;DR: In this article, the structure of Schiff base and polymer complexes have been characterized by elemental analysis, spectral (FT-IR, UV-Vis, 1H NMR and ESR), X-ray diffraction, magnetic moment measurements and molar conductance.
Journal ArticleDOI
Synthesis, Characterization, and Antibacterial and Cytotoxic Study of Metal Complexes with Schiff Base Ligands
TL;DR: Among the compounds tested, the cobalt complexes 1a, 2a, 3a, and 4a showed the most favourable antibacterial and cytotoxic activities.
References
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5-(3-carboxymethoxyphenyl)-2-(4,5-dimethylthiazolyl)-3-(4-sulfophenyl)tetrazolium, inner salt (MTS) and related analogs of 3-(4,5-dimethylthiazolyl)-2,5-diphenyltetrazolium bromide (MTT) reducing to purple water-soluble formazans As cell-viability indicators
TL;DR: Analogs of MTT, 3-(4,5-dimethylthiazolyl)-2,5diphenyltetrazolium bromide, designed to yield water-soluble formazans upon reduction, have been synthesized and evaluated as cell-viability indicators as mentioned in this paper.
Journal ArticleDOI
Resveratrol, a remarkable inhibitor of ribonucleotide reductase.
TL;DR: It is shown that Resveratrol is a remarkable inhibitor of ribonucleotide reductase and DNA synthesis in mammalian cells, which might have further applications as an antiproliferative or a cancer chemopreventive agent in humans.
Journal ArticleDOI
Triapine (3-aminopyridine-2-carboxaldehyde- thiosemicarbazone): A potent inhibitor of ribonucleotide reductase activity with broad spectrum antitumor activity
Rick Avery Finch,M.‐C. Liu,Susan P. Grill,William C. Rose,Regina Loomis,Karen M. Vasquez,Yung-Chi Cheng,Alan C. Sartorelli +7 more
TL;DR: The findings demonstrate the superiority of Triapine over hydroxyurea as an anticancer agent and suggest that prevention byTriapine of repair of DNA lesions created by agents that damage DNA may result in efficacious drug combinations for the treatment of cancer.
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Use of an aqueous soluble tetrazolium/formazan assay to measure viability and proliferation of lymphokine-dependent cell lines
TL;DR: Its advantages over XTT/PMS, another tetrazolium which yields a water-soluble formazan product, include the absorbance range of color produced, the rapidity of color development, and the storage stability of the MTS/P MS reagent solution.
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The Measurement of Partition Coefficients
John C. Dearden,G. M. Bresnen +1 more
TL;DR: In this paper, the authors examined the factors that can affect the measurement of partition coefficient, and made recommendations as to good practice, and recommended that partitioning be carried out at constant temperature using either a stirred flask technique or the filter probe.