2. Academic Validation
  3. Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110alpha inhibitors

Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110alpha inhibitors

  • Bioorg Med Chem. 2006 Oct 15;14(20):6847-58. doi: 10.1016/j.bmc.2006.06.046.
Masahiko Hayakawa 1,  Hiroyuki Kaizawa,  Hiroyuki Moritomo,  Tomonobu Koizumi,  Takahide Ohishi,  Minoru Okada,  Mitsuaki Ohta,  Shin-ichi Tsukamoto,  Peter Parker,  Paul Workman,  Mike Waterfield
Affiliations

Affiliation

  • 1 Institute for Drug Discovery Research, Astellas Pharma Inc., Tsukuba, Ibaraki 300-2698, Japan. masahiko.hayakawa@jp.astellas.com
PMID: 16837202 DOI: 10.1016/j.bmc.2006.06.046
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.

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