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Bioorg Med Chem Lett. 2011 Aug 15;21(16):4773-8. doi: 10.1016/j.bmcl.2011.06.063. Epub 2011 Jun 21.

Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.

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1
Medicinal Chemistry, Pfizer, 401 N. Middletown Rd., Pearl River, NY 10965, USA. christoph.dehnhardt@pfizer.com

Abstract

We recently described several highly potent, triazine (1) and triazolopyrimidine (2) scaffold-based, dual PI3K/mTOR-inhibitors (e.g., 1, PKI-587) that were efficacious in both in vitro and in vivo models. In order to further optimize these compounds we devised a novel series, the 2-oxatriazines, which also exhibited excellent potency and good metabolic stability. Some 2-oxatriazines showed promising in vivo biomarker suppression and induced apoptosis in the MDA-MB-361 breast cancer xenograft model.

PMID:
21763134
DOI:
10.1016/j.bmcl.2011.06.063
[Indexed for MEDLINE]
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