Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 60, Issue -, Pages 187-198Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.12.004
Keywords
Coumarins; Pyrazoline; Phenylsulfonyl derivatives; Antitumor activity
Categories
Funding
- Cairo University [1999/45 a]
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Two groups of coumarin pyrazoline hybrids were synthesized. The target compounds were obtained by cyclization of the coumarin chalcones with various substituted hydrazines to produce the corresponding pyrazolines through 1,4-addition on alpha,beta-unsaturated carbonyl system. Selected compounds were investigated for their anticancer activity toward 60 cancer cell lines according to US NCI protocol where breast cancer MCF7 and colon cancer HCT-116 were the most susceptible to the influence of compounds 7d, 8c and 9c. Encouraged by this, all final compounds were screened against colorectal cell line HCT-116. The tested compounds exhibited high potency with IC50 ranging from 0.01 mu M to 2.8 mu M. Moreover, compound 9c which possessed the highest cytotoxicity proved to have weak enzyme inhibitory activity against PI3K (p110 alpha/p85 alpha). (C) 2012 Elsevier Masson SAS. All rights reserved.
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