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Bioorg Med Chem Lett. 2011 Jul 1;21(13):4036-40. doi: 10.1016/j.bmcl.2011.04.129. Epub 2011 May 7.

Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability.

Author information

1
Department of Cancer Biology, Dana Farber Cancer Institute, 44 Binney Street, Boston, MA 02115, USA.

Abstract

Starting from small molecule mTOR inhibitor Torin1, replacement of the piperazine ring with a phenyl ring resulted in a new series of mTOR inhibitors (as exemplified by 10) that showed superior potency and selectivity for mTOR, along with significantly improved mouse liver microsome stability and a longer in vivo half-life.

PMID:
21621413
PMCID:
PMC3929239
DOI:
10.1016/j.bmcl.2011.04.129
[Indexed for MEDLINE]
Free PMC Article

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