Literature DB >> 23122859

Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase γ inhibitors.

Yusuke Oka1, Tetsuya Yabuuchi, Yasuyuki Fujii, Hidenori Ohtake, Shunichi Wakahara, Kayo Matsumoto, Mayumi Endo, Yunoshin Tamura, Yoshinori Sekiguchi.   

Abstract

A novel series of 2-aminothiazole-oxazoles was designed and synthesized as part of efforts to develop potent phosphoinositide 3-kinase γ (PI3Kγ) inhibitors. The modification of a high-throughput screening hit, compound 1, resulted in the identification of compounds 10 and 15, which displayed potent inhibitory activities in enzyme-based and cell-based assays.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23122859     DOI: 10.1016/j.bmcl.2012.10.028

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

Review 1.  Recent syntheses of PI3K/Akt/mTOR signaling pathway inhibitors.

Authors:  Mark E Welker; George Kulik
Journal:  Bioorg Med Chem       Date:  2013-05-09       Impact factor: 3.641

Review 2.  Recent development of ATP-competitive small molecule phosphatidylinostitol-3-kinase inhibitors as anticancer agents.

Authors:  Yu Liu; Wen-Zhu Wan; Yan Li; Guan-Lian Zhou; Xin-Guang Liu
Journal:  Oncotarget       Date:  2017-01-24
  2 in total

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