Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 8, Pages 1907-1911Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.03.011
Keywords
Multisubstituted indole-acrylonitrile; Hybrids; Synthesis; Cytotoxic activity
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Funding
- Projects in the National Science & Technology Pillar Program [2011BAE06B004-02, 2011BAE06B004-15]
- Hubei Agricultural Science Innovation Centre [2012-620-008-002]
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A series of multisubstituted indole-acrylonitrile hybrids were designed, synthesized and evaluated for their potential cytotoxic activities. The bio-evaluation results indicated that some of the target compounds (such as 3a, 3f, 3k, 3n) exhibited good to moderate cytotoxic effect on HepG2, BCG-823, BEL7402, and HL-7702 cell lines. Especially, the compounds 3a and 3k also exhibited high cytotoxic activities (3a, 19.38 +/- 3.38 mu M; 3k, 15.43 +/- 3.54 mu M) against the BEL-7402 cell line resistant to Taxol (>25 mu M) and 5-FU (>500 mu M), which might be developed as novel lead scaffold for potential anticancer agents. (c) 2014 Elsevier Ltd. All rights reserved.
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