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Synthesis and biological evaluation of novel coumarin-pyrazoline hybrids endowed with phenylsulfonyl moiety as antitumor agents.

Abstract：

: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 α,β-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 IC(50) ranging from 0.01 μM to 2.8 μM. Moreover, compound 9c which possessed the highest cytotoxicity proved to have weak enzyme inhibitory activity against PI3K (p110α/p85α).

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Amin KM,Eissa AA,Abou-Seri SM,Awadallah FM,Hassan GS

doi

10.1016/j.ejmech.2012.12.004

subject

Has Abstract

pub_date

2013-02-01 00:00:00

pages

187-98

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00726-X

journal_volume

60

pub_type

杂志文章

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