期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 17, 页码 4980-4983出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.070
关键词
beta-Catenin/Tcf-4 pathway; Inhibitors; 2,4-Diamino-quinazoline
The synthesis and SAR of a series of 2,4-diamino-quinazoline derivatives as beta-catenin/Tcf-4 inhibitors are described. This series was developed by modifying the initial lead 1, which was identified by screening of our compound library and found to inhibit the beta-catenin/Tcf-4 pathway. Replacement of the biphenyl moiety in compound 1 with the N-phenylpiperidine-4-carboxamide chain as in 2, resulted in a number of new analogues, which are potent inhibitors of the beta-catenin/Tcf-4 pathway. Compound such as 16k exhibited good cellular potency, solubility, metabolic stability and oral bioavailability. (C) 2009 Elsevier Ltd. All rights reserved.
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