4.5 Article

Synthesis and biological evaluation of matrine derivatives as anti-hepatocellular cancer agents

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 17, Pages 4267-4271

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.07.045

Keywords

Matrine derivatives; Hepatocarcinoma; Anticancer activity; Cell cycle; Migration

Funding

  1. National Natural Science Foundation of China [21262005]
  2. high level innovation team and outstanding scholar project of Guangxi institutions of higher education [[2014] 49]
  3. Postdoctoral Science Foundation of Guangxi province of China

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We delineate herein the synthesis and anti-cancer effects of 15 matrine derivatives. The in vitro growth inhibitory assays showed that most of the prepared compounds exhibited improved anti-proliferative activities towards cancer cells with IC50 17-109 times lower than that of matrine. Compounds CH6 showed the most potent anti-proliferative activities in the four tested cancer cell lines. Moreover, compound CH6 could induce G1 cell cycle arrest and inhibit cell migration in human hepatocellular cancer cell lines Bel-7402 and HepG2 through up-regulation of P21, P27 and E-cadherin and down-regulation of N-cadherin. (C) 2016 Elsevier Ltd. All rights reserved.

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