Design, synthesis, and biological evaluation of new diaminoquinazolines as β-catenin/Tcf4 pathway inhibitors

…, N Lin, W Tian, X Han, X Han, Z Huang…

Index: Mao, Yongjun; Lin, Nan; Tian, Wang; Han, Xiaofeng; Han, Xiaobing; Huang, Ziwei; An, Jing Journal of Medicinal Chemistry, 2012 , vol. 55, # 3 p. 1346 - 1359

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Citation Number: 4

Abstract

More than 50 new diaminoquinazoline derivatives have been synthesized and evaluated in a colon carcinoma cell growth inhibition assay using HCT116 and SW480 cells. Twenty compounds with good cell growth inhibitory activities (< 4 μM) were tested as inhibitors of the β-catenin/T cell transcription factor 4 (Tcf4) signaling pathway using a HCT116 cell- based luciferase reporter assay. Results from the biological activities as well as the ...