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Bioorg Med Chem Lett. 2010 Apr 15;20(8):2654-7. doi: 10.1016/j.bmcl.2010.02.029. Epub 2010 Feb 11.

Triazines incorporating (R)-3-methylmorpholine are potent inhibitors of the mammalian target of rapamycin (mTOR) with selectivity over PI3Kalpha.

Author information

1
Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA. david.j.richard@pfizer.com

Abstract

Potent inhibitors of the mammalian target of rapamycin (mTOR) which contain the triazine scaffold and the (R)-3-methyl morpholine moiety have been identified. Such compounds also demonstrated good selectivity over the related lipid kinase PI3Kalpha. Incorporation of additional functionality at the 4-position of the arylureidophenyl ring resulted in compounds with enhanced cellular activity.

PMID:
20223664
DOI:
10.1016/j.bmcl.2010.02.029
[Indexed for MEDLINE]

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