Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 15, Pages 4297-4302Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.06.001
Keywords
Hybrid compound; Benzofuran; Imidazole; Triazole; Structure-activity relationships
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Funding
- NSFC [30960460, 20925205, 21062026]
- NSFYN [2010GA014, 2012FB113]
- PRTTSTYN [2009C1120]
- NBRPC (973 Program) [2009CB522300]
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A series of novel hybrid compounds of 2-phenyl-3-alkylbenzofuran and imidazole or triazole were prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the 2-ethyl-imidazole ring, and substitution of the imidazolyl-3-position with a 2-bromobenzyl or naphthylacyl group, were vital for modulating inhibitory activity. In particular, hybrid compound 31 was found to be the most potent derivative with IC50 values of 0.08-0.55 mu M against five strains human tumor cell lines and was found to be more selective against breast carcinoma (MCF-7) and colon carcinoma (SW480) (IC50 values 40.8-fold and 40.1-fold lower than cisplatin (DDP)). (C) 2013 Elsevier Ltd. All rights reserved.
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