Synthesis, Biological Evaluation, and Quantitative Structure−Activity Relationship Analysis of New Schiff Bases of Hydroxysemicarbazide as Potential Antitumor Agents†
作者： Shijun Ren , Rubin Wang , Kenichi Komatsu , Patricia Bonaz-Krause , Yegor Zyrianov
DOI: 10.1021/JM010252Q
关键词:
摘要: 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 9.4 10-4 M. A total 17 out the 30 compounds had higher inhibitory activities than hydroxyurea (an anticancer drug currently used for treatment melanoma, leukemia, ovarian cancer) Six with micromolar 11- 30-fold more potent (IC50 = 8.2 10-5 M). partition coefficient (log P) ionization constants (pKa) model compound [1-(3-trifluoromethylbenzylidene)-4-hydroxysemicarbazide, 1] measured by shake-flask method, log P was derive Hansch−Fujita π constant −CHNNHCONHOH. On basis newly derived those other moieties, coefficients (SlogP) 29 calculated summation values. Quantitative structure−activity relations...
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