4.5 Article

Design, synthesis and cytotoxic activities of novel hybrid compounds between 2-phenylbenzofuran and imidazole

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 8, Pages 2726-2729

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.02.094

Keywords

Hybrid compound; Benzofuran; Imidazole; Cytotoxic activities; Structure-activity relationships

Funding

  1. National Natural Science Foundation of China [30960460, 21062026, 2010GA014, 2009CB522300]
  2. Yunnan Province
  3. National Basic Research Program of China (973 Program)

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A series of novel hybrid compounds between 2-phenylbenzofuran and imidazole have been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that substitution of the imidazolyl-3-position with a naphthylacyl or bromophenacyl group, were vital for modulating cytotoxic activity. In particular, hybrid compound 15 was found to be the most potent compound against 4 strains human tumor cell lines and more active than cisplatin (DDP), and exhibited cytotoxic activity selectively against liver carcinoma (SMMC-7721). (C) 2012 Elsevier Ltd. All rights reserved.

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