Synthesis and In-Vitro Cytotoxicity of (E)-N,2,3-Triarylacrylamide Derivatives as Analogs of Combretastatin A-4

Title:Synthesis and In-Vitro Cytotoxicity of (E)-N,2,3-Triarylacrylamide Derivatives as Analogs of Combretastatin A-4

Volume: 11 Issue: 5

Author(s): Kun-Ming Jiang, Xiao-Li Dai, Ke Li, Di Wu, Ji-Hong Zhang, Yi Jin and Jun Lin

Affiliation:

Keywords: Cytotoxic activity, (E)-N, 2, 3-triarylacrylamide, SARs, synthesis.

Abstract: A new series of (E)-N,2,3-triarylacrylamide derivatives were designed and synthesized as potent anticancer agents. Cytotoxicity of the 26 target compounds was evaluated in vitro against six cancer cell lines (HCT116, A549, MDA-MB-468, HepG2, SKNMC and SK-OV-3) by Sulforhodamine B colorimetric assay. The most promising compound, 4h, was as potent as the reference drug cisplatin (DDP). Preliminary structure–activity relationship (SAR) data provided guidance for further design and discovery of (E)- N,2,3-triarylacrylamide scaffold anticancer agents.

Cite this article as:

Jiang Kun-Ming, Dai Xiao-Li, Li Ke, Wu Di, Zhang Ji-Hong, Jin Yi and Lin Jun, Synthesis and In-Vitro Cytotoxicity of (E)-N,2,3-Triarylacrylamide Derivatives as Analogs of Combretastatin A-4, Medicinal Chemistry 2015; 11 (5) . https://dx.doi.org/10.2174/1573406410666141226132926