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

被引：0

作者：

Jiang, Kun-Ming ^{[1
]}

Dai, Xiao-Li ^{[2
]}

Li, Ke ^{[3
]}

Wu, Di ^{[1
]}

Zhang, Ji-Hong ^{[2
]}

Jin, Yi ^{[1
]}

Lin, Jun ^{[1
]}

机构：

[1] Yunnan Univ, Sch Chem Sci & Technol, Lab Med Chem Nat Resource, Minist Educ, Kunming 650091, Peoples R China

[2] Kunming Univ Sci & Technol, Fac Life Sci & Technol, Kunming 650224, Peoples R China

[3] Kunming Med Univ, Affiliated Hosp 3, Dept Med Oncol 1, Kunming 650031, Peoples R China

来源：

MEDICINAL CHEMISTRY | 2015年 / 11卷 / 05期

关键词：

Cytotoxic activity; (E)-N,2,3-triarylacrylamide; SARs; synthesis; TUBULIN; AGENTS; GROWTH; CANCER; A4;

D O I：

10.2174/1573406410666141226132926

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：453 / 461

页数：9

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