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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Synthesis of new Schiff bases bearing 1,2,4-triazole, thiazolidine and chloroazetidine moieties and their pharmacological evaluation
TL;DR: In vitro antimicrobial activity of the new compounds was evaluated using a broth dilution technique and revealed data showed that compound 9d has excellent activity against Gram + ve and Gram –ve bacteria, and compounds 11b presented promising anticancer activity against HELA cervix.
Journal ArticleDOI
Synthesis, spectroscopic and thermal studies of some IIB group complexes with a new N2-Schiff base ligand
TL;DR: The thermal behavior of the complexes shows weight loss by decomposition of the anions and ligand segments in the subsequent steps and activation thermodynamic parameters of decomposition such as E*, ΔH*, ΔS* and ΔG* were calculated from TG curves.
Journal ArticleDOI
Novel semicarbazides and ureas of primaquine with bulky aryl or hydroxyalkyl substituents: synthesis, cytostatic and antioxidative activity.
Kristina Pavić,Ivana Perković,Matej Cindrić,Mateja Pranjić,Irena Martin-Kleiner,Marijeta Kralj,Dominique Schols,Dimitra Hadjipavlou-Litina,Ana Maria Katsori,Branka Zorc +9 more
TL;DR: All primaquine semicarbazide derivatives showed either prominent cytostatic activity towards all the tested cell lines or high selectivity towards MCF-7 cells, with IC50 values in the low micromolar range.
Journal ArticleDOI
Development of Ribonucleotide Reductase Inhibitors: A Review on Structure Activity Relationships
TL;DR: This review concluded that RNR inhibitors composed of different fragments such as aryl, heteroaryl, sugar moiety, polar groups, flexible bonds, etc which are required for the binding of the molecules to the RNR enzymes can provide significant novel molecules with acceptable pharmacokinetic properties.
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Endosomal pH responsive polymers for efficient cancer targeted gene therapy
TL;DR: The FA-SLICS has negligible cytotoxicity to normal cells (CHO), but displays slight toxicity to cancer cells (HeLa and HepG2), and should be a promising delivery vector in cancer gene therapy based on its cell targeting capability and intracellular microenvironment controlled delivery mechanism.
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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.
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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.
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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.