Title of article
Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110α inhibitors Original Research Article
Author/Authors
Masahiko Hayakawa، نويسنده , , Hiroyuki Kaizawa، نويسنده , , Hiroyuki Moritomo، نويسنده , , Tomonobu Koizumi، نويسنده , , Takahide Ohishi، نويسنده , , Minoru Okada، نويسنده , , Mitsuaki Ohta، نويسنده , , Shin-ichi Tsukamoto، نويسنده , , Peter Parker، نويسنده , , Paul Workman، نويسنده , , Mike Waterfield، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
12
From page
6847
To page
6858
Abstract
A series of 4-morpholino-2-phenylquinazolines and related derivatives were prepared and evaluated as inhibitors of PI3 kinase p110α. In this series, the thieno[3,2-d]pyrimidine derivative 15e showed the strongest inhibitory activity against p110α, with an IC50 value of 2.0 nM, and inhibited proliferation of A375 melanoma cells with an IC50 value of 0.58 μM. Moreover, 15e was found to be selective for p110α over other PI3K isoforms and protein kinases, making it the first example of a selective PI3K p110α inhibitor.
Keywords
p110? , Inhibitor , Cancer treatment , PI3 kinase
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2006
Journal title
Bioorganic and Medicinal Chemistry
Record number
1305176
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