title: Multisubstituted indole-acrylonitrile hybrids as potential cytotoxic agents.
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.
authors.affiliation: National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China. Electronic address: keshaoyong@163.com.
authors.forename: Shaoyong
authors.initials: S
authors.lastname: Ke
authors.affiliation: National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China.
authors.forename: Ziwen
authors.initials: Z
authors.lastname: Yang
authors.affiliation: National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China.
authors.forename: Zhigang
authors.initials: Z
authors.lastname: Zhang
authors.affiliation: National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Liang
authors.affiliation: National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China.
authors.forename: Kaimei
authors.initials: K
authors.lastname: Wang
authors.affiliation: National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China.
authors.forename: Manli
authors.initials: M
authors.lastname: Liu
authors.affiliation: National Biopesticide Engineering Research Center, Hubei Academy of Agricultural Sciences, Wuhan 430064, People's Republic of China. Electronic address: shiliqiao_75@163.com.
authors.forename: Liqiao
authors.initials: L
authors.lastname: Shi
mesh_terms: D000181:Acrylonitrile / Q000737:chemistry / Q000633:toxicity; D000970:Antineoplastic Agents / Q000737:chemistry / Q000633:toxicity; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003603:Cytotoxins / Q000737:chemistry / Q000633:toxicity; D019008:Drug Resistance, Neoplasm / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D056945:Hep G2 Cells; D006801:Humans; D007211:Indoles / Q000737:chemistry / Q000633:toxicity; D020128:Inhibitory Concentration 50; D015394:Molecular Structure
chemical_list: D000970:Antineoplastic Agents; D003603:Cytotoxins; D007211:Indoles; C030374:indole; D000181:Acrylonitrile
keywords: Cytotoxic activity; Hybrids; Multisubstituted indole–acrylonitrile; Synthesis