2. Academic Validation
  3. Synthesis and evaluation of novel 7-azaindazolyl-indolyl-maleimide derivatives as antitumor agents and protein kinase C inhibitors

Synthesis and evaluation of novel 7-azaindazolyl-indolyl-maleimide derivatives as antitumor agents and protein kinase C inhibitors

  • Bioorg Med Chem. 2009 Jul 1;17(13):4763-72. doi: 10.1016/j.bmc.2009.04.043.
Qing Ye 1,  Ji Cao,  Xinglu Zhou,  Dan Lv,  Qiaojun He,  Bo Yang,  Yongzhou Hu
Affiliations

Affiliation

  • 1 ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
PMID: 19447039 DOI: 10.1016/j.bmc.2009.04.043
Abstract

A series of novel 7-azaindazolyl-indolyl-maleimides were synthesized and evaluated for their antiproliferative activity in vitro against various human Cancer cell lines and protein kinase C inhibitory activity. Compounds 8a-c, 8e and 14a were the most promising compounds against K562, A549, ECA-109, KB and SMMC-7721 cell lines in vitro. Compounds 9a-j showed moderate PKC inhibition. Further mechanism of action studies revealed that the antiproliferative activity of compound 8b in KB cells might involve the mitochondria-mediated Apoptosis pathway.

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