Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors.

Gilles Ouvry,Laurence Clary,Loïc Tomas,Michèle Aurelly,Laetitia Bonnary, Emilie Borde,Claire Bouix-Peter, Laurent Chantalat, Claire Defoin-Platel,Sophie Deret,Mathieu Forissier,Craig S Harris,Tatiana Isabet,Laurent Lamy,Anne-Pascale Luzy, Jonathan Pascau, Catherine Soulet, Alessandro Taddei, Nathalie Taquet, Etienne Thoreau, Emeric Varvier,Emmanuel Vial,Laurent F Hennequin

ACS medicinal chemistry letters（2019）

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摘要

Minor structural modifications-sometimes single atom changes-can have a dramatic impact on the properties of compounds. This is illustrated here on structures related to known mTOR inhibitor Sapanisertib. Subtle changes in the hinge binder lead to strikingly different overall profiles with changes in physical properties, metabolism, and kinase selectivity.

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关键词

mTOR,kinase,selectivity,metabolism,topical application

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