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

Index: Eur. J. Med. Chem. 46 , 5868-77, (2011)

Full Text: HTML

Abstract

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.

Related Compounds

  • Fluorouracil
  • carbohydrazide

Related Articles:

TAp73 promotes cell survival upon genotoxic stress by inhibiting p53 activity.

2014-09-30

[Oncotarget 5(18) , 8107-22, (2014)]

cIEF for rapid pKa determination of small molecules: a proof of concept.

2014-10-15

[Eur. J. Pharm. Sci. 63 , 14-21, (2014)]

Establishment and characterization of cell lines from chromosomal instable colorectal cancer.

2015-01-07

[World J. Gastroenterol. 21(1) , 164-76, (2015)]

Targeted Delivery of 5-fluorouracil with Monoclonal Antibody Modified Bovine Serum Albumin Nanoparticles.

[Iran. J. Pharm. Res. 14(2) , 395-405, (2015)]

Atonal homolog 1 protein stabilized by tumor necrosis factor α induces high malignant potential in colon cancer cell line.

2015-08-01

[Cancer Sci. 106 , 1000-7, (2015)]

More Articles...