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

Alessandro Taddei (7473296); Anne-Pascale Luzy (5025623); Catherine Soulet (7473293); Claire Bouix-Peter (3075795); Claire Defoin-Platel (7473281); Craig S. Harris (2170579); Emeric Varvier (7473302); Emilie Borde (7473278); Emmanuel Vial (7473305); Etienne Thoreau (7473299); Gilles Ouvry (2832038); Jonathan Pascau (5134760); Laetitia Bonnary (7473275); Laurence Clary (5134790); Laurent Chantalat (5134745); Laurent F. Hennequin (2521291); Laurent Lamy (7473290); Loïc Tomas (7473272); Mathieu Forissier (7473287); Michèle Aurelly (5134748); Nathalie Taquet (342878); Sophie Deret (7473284); Tatiana Isabet (5134796)

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

Abstract

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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Last time updated on 06/04/2020