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

Qingsong Liu, Jinhua Wang, Seong A. Kang, Carson C. Thoreen, Wooyoung Hur, Hwan Geun Choi, David L. Waller, Taebo Sim, David M. Sabatini, Nathanael S. Gray

Research output: Contribution to journalArticle

9 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)4036-4040
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number13
DOIs
Publication statusPublished - 2011 Jul 1

Keywords

  • PI3K
  • Torin1
  • mTOR

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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