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

[ Vol. 11 , Issue. 5 ]

Author(s):

Kun-Ming Jiang, Xiao-Li Dai, Ke Li, Di Wu, Ji-Hong Zhang, Yi Jin and Jun Lin   Pages 453 - 461 ( 9 )

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.

Keywords:

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

Affiliation:

Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University), Ministry Education, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, P.R. China., Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University), Ministry Education, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, P.R. China.

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