| Literature DB >> 16837202 |
Masahiko Hayakawa1, Hiroyuki Kaizawa, Hiroyuki Moritomo, Tomonobu Koizumi, Takahide Ohishi, Minoru Okada, Mitsuaki Ohta, Shin-ichi Tsukamoto, Peter Parker, Paul Workman, Mike Waterfield.
Abstract
A series of 4-morpholino-2-phenylquinazolines and related derivatives were prepared and evaluated as inhibitors of PI3 kinase p110alpha. In this series, the thieno[3,2-d]pyrimidine derivative 15e showed the strongest inhibitory activity against p110alpha, with an IC(50) value of 2.0 nM, and inhibited proliferation of A375 melanoma cells with an IC(50) value of 0.58 microM. Moreover, 15e was found to be selective for p110alpha over other PI3K isoforms and protein kinases, making it the first example of a selective PI3K p110alpha inhibitor.Entities:
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Year: 2006 PMID： 16837202 DOI： 10.1016/j.bmc.2006.06.046
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641