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Synthesis and biological evaluation of 2-phenylthiazole-4-carboxamide derivatives as anticancer agents.

Abstract：

:A series of substituted 2-phenylthiazole-4-carboxamide derivatives were synthesized as potential cytotoxic agents and evaluated against three human cancer cell lines including T47D (Breast cancer), Caco-2 (Colorectal cancer) and HT-29 (Colon cancer). The SAR of the arylacetamido pendent connected to the para-position of 2-phenylthiazole were explored. It was found that substitution at the 4-position by a methoxy group led to improvement of activity against Caco-2 cells while 2-methoxy substituent could maintain the high activity against HT-29 and T47D cell lines. Also, 3-fluoro analog showed good cytotoxic activity profile against all cell lines with IC(50) values less than 10 μg/mL.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Aliabadi A,Shamsa F,Ostad SN,Emami S,Shafiee A,Davoodi J,Foroumadi A

doi

10.1016/j.ejmech.2010.08.063

subject

Has Abstract

pub_date

2010-11-01 00:00:00

pages

5384-9

issue

11

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(10)00644-6

journal_volume

45

pub_type

杂志文章

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