| Literature DB >> 19640711 |
Zecheng Chen1, Aranapakam M Venkatesan, Christoph M Dehnhardt, Osvaldo Dos Santos, Efren Delos Santos, Semiramis Ayral-Kaloustian, Lei Chen, Yi Geng, Kim T Arndt, Judy Lucas, Inder Chaudhary, Tarek S Mansour.
Abstract
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.Entities:
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Year: 2009 PMID： 19640711 DOI： 10.1016/j.bmcl.2009.07.070
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823