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ID: ALA1152933

Journal: Bioorg Med Chem

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

Authors: Ye Q, Cao J, Zhou X, Lv D, He Q, Yang B, Hu Y.

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.

CiteXplore: 19447039

DOI: 10.1016/j.bmc.2009.04.043