Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2006 Oct 15;14(20):6847-58.
doi: 10.1016/j.bmc.2006.06.046. Epub 2006 Jul 11.

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

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

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

Masahiko Hayakawa et al. Bioorg Med Chem. .

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.

PubMed Disclaimer

MeSH terms

LinkOut - more resources