Design, synthesis and biological activities of quinazoline containing sorafenib analogs as antitumor agents

Jingwen Zhang, Ningning Wang, Xiaoxia Xie, Chunhong Yan, Fenghua Fu, Jianwen Yao, Hongbo Wang

Research output: Contribution to journalArticle

1 Scopus citations

Abstract

A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their antiproliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the synthesized compounds showed significant cytotoxicity against the selected cell lines. These cytotoxicities were consistent with their inhibitory activity against the phosphorylation of c-Raf, MEK1/2 and ERK1/2. Compound GD-09 also showed much stronger anti-tumor activity than that of sorafenib in vivo by B16 melanoma xenograft model test.

Original languageEnglish (US)
Pages (from-to)239-246
Number of pages8
JournalWuhan University Journal of Natural Sciences
Volume22
Issue number3
DOIs
StatePublished - Jun 1 2017

Keywords

  • antitumor agents
  • quinazoline
  • sorafenib analogs
  • synthesis

ASJC Scopus subject areas

  • General

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