Multisubstituted indole-acrylonitrile hybrids as potential cytotoxic agents

  • Bioorg Med Chem Lett. 2014 Apr 15;24(8):1907-11. doi: 10.1016/j.bmcl.2014.03.011.
Shaoyong Ke  1 ,  Ziwen Yang  2 ,  Zhigang Zhang  2 ,  Ying Liang  2 ,  Kaimei Wang  2 ,  Manli Liu  2 ,  Liqiao Shi  3
Affiliations
  • 1. National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China. Electronic address: [email protected].
  • 2. National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China.
  • 3. National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China. Electronic address: [email protected].
PMID: 24684840 DOI: 10.1016/j.bmcl.2014.03.011
Abstract

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, BEL-7402, and HL-7702 cell lines. Especially, the compounds 3a and 3k also exhibited high cytotoxic activities (3a, 19.38±3.38 μM; 3k, 15.43±3.54 μM) against the BEL-7402 cell line resistant to Taxol (>25μM) and 5-FU (>500 μM), which might be developed as novel lead scaffold for potential Anticancer agents.

Keywords
Cytotoxic activity; Hybrids; Multisubstituted indole–acrylonitrile; Synthesis.