Analogues and derivatives of oncrasin-1, a novel inhibitor of the C-terminal domain of RNA polymerase II and their antitumor activities

…, L Wang, W Guo, X Liu, J Liu, X Wei…

Index: Wu, Shuhong; Wang, Li; Guo, Wei; Liu, Xiaoying; Liu, Jinsong; Wei, Xiaoli; Fang, Bingliang Journal of Medicinal Chemistry, 2011 , vol. 54, # 8 p. 2668 - 2679

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Citation Number: 29

Abstract

To optimize the antitumor activity of oncrasin-1, a small molecule RNA polymerase II inhibitor, we evaluated 69 oncrasin-1 analogues for their cytotoxic activity against normal human epithelial cells and K-Ras mutant tumor cells. About 40 of those compounds were as potent as or more potent than oncrasin-1 in tumor cells and had a minimal cytotoxic effect on normal cells. Structure− activity relationship analysis revealed that most of the active ...