European Journal of Medicinal Chemistry 2011-12-01

Synthesis and cytotoxic activity of novel 3-(1H-indol-3-yl)-1H-pyrazole-5-carbohydrazide derivatives.

Datong Zhang, Guangtian Wang, Guilong Zhao, Weiren Xu, Lingyan Huo, Datong Zhang, Guangtian Wang, Guilong Zhao, Weiren Xu, Lingyan Huo

文献索引：Eur. J. Med. Chem. 46 , 5868-77, (2011)

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摘要

A series of novel 3-(1H-indole-3-yl)-1H-pyrazole-5-carbohydrazide derivatives 4Ia-n, 4IIa-b and 6 were prepared by hydrazinolysis of ethyl 3-(1H-indole-3-yl)-1H-pyrazole-5-carboxylate with hydrazine hydrate in excellent yields. These new compounds were fully characterized by spectroscopic methods, and the important intermediates 3Ie, 3IIc and 3IId were further confirmed by X-ray crystallography. All the new compounds were evaluated for their cytotoxic activity against 4 human cancer cell lines by MTT method. Some of them exhibited more potent antiproliferative activity against HepG-2, BGC823 and BT474 cell lines than the positive drug 5-fluorourcail. Flow cytometry analysis showed that 4Ik and 4Il arrested the cell cycle at S phase.Copyright © 2011 Elsevier Masson SAS. All rights reserved.