Development of erlotinib derivatives as CIP2A-ablating agents independent of EGFR activity

…, CY Liu, HJ Chen, JW Huang, IK Kim, CW Shiau

Index: Chen, Kuen-Feng; Pao, Kuan-Chuan; Su, Jung-Chen; Chou, Yi-Chieh; Liu, Chun-Yu; Chen, Hui-Ju; Huang, Jui-Wen; Kim, Inki; Shiau, Chung-Wai Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 20 p. 6144 - 6153

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Citation Number: 20

Abstract

Cancerous inhibitor of PP2A (CIP2A) is a novel human oncoprotein that inhibits PP2A, contributing to tumor aggressiveness in various cancers. Several studies have shown that downregulation of CIP2A by small molecules reduces PP2A-dependent phosphorylation of Akt and induces cell death. Here, a series of mono-and di-substituted quinazoline and pyrimidine derivatives based on the skeleton of erlotinib (an EGFR inhibitor) were ...