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Bioorg Med Chem Lett. 2011 Feb 15;21(4):1270-4. doi: 10.1016/j.bmcl.2010.12.026. Epub 2010 Dec 10.

Quinazolines with intra-molecular hydrogen bonding scaffold (iMHBS) as PI3K/mTOR dual inhibitors.

Author information

1
Pfizer Global Research and Development, Chemistry Department, 10770 Science Center Drive, La Jolla, CA 92120, USA. Kevin.K.Liu@pfizer.com

Abstract

Intra-molecular hydrogen bonding was introduced to the quinazoline motif to form a pseudo ring (intra-molecular H-bond scaffold, iMHBS) to mimic our previous published core structures, pyrido[2.3-D]pyrimidin-7-one and pteridinone, as PI3K/mTOR dual inhibitors. This design results in potent PI3K/mTOR dual inhibitors and the purposed intra-molecular hydrogen bonding structure is well supported by co-crystal structure in PI3Kγ enzyme. In addition, a novel synthetic route was developed for these analogs.

PMID:
21269826
DOI:
10.1016/j.bmcl.2010.12.026
[Indexed for MEDLINE]

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