4.5 Article

Rational discovery of a highly novel and selective mTOR inhibitor

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 29, Issue 21, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.126659

Keywords

mTOR; SBDD; Inhibitor

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Aided by Structure Based Drug Discovery (SBDD), we rapidly designed a highly novel and selective series of mTOR inhibitors. This chemotype conveys exquisite kinase selectivity, excellent in vitro and in vivo potencies and ADME safety profiles. These compounds could serve as good tools to explore the potential of TORC inhibition in various human diseases.

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