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Article

Design and Synthesis of Novel Diaminoquinazolines with <i>in Vivo</i> Efficacy for β-Catenin/T-Cell Transcriptional Factor 4 Pathway Inhibition

21 Dec 2009

Abstract excerpt

We are introducing a novel series of 2,4-diaminoquinazolines as beta-catenin/Tcf4 inhibitors which were identified by ligand-based design. Here we elucidate the SAR of this series and explain how we were able to improve key molecular properties such as solubility and cLogP leading to compound 9. Analogue 9 exhibited better biological activity and improved physical and pharmacological properties relative to the...

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PMID: 20025292
DOI: 10.1021/jm901370m

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