A Simple Isomerization of the Purine Scaffold of a Kinase Inhibitor, Roscovitine, Affords a Four- to Seven-Fold Enhancement of Its Affinity for Four CDKs. Could This Be Traced Back to Conjugation-Induced Stiffenings/Loosenings of Rotational Barriers?

Bibliographic Details
Main Authors: Krystel El Hage, Jean-Philip Piquemal, Nassima Oumata, Laurent Meijer, Hervé Galons, Nohad Gresh
Format: Article
Language:English
Published: American Chemical Society 2017-07-01
Series:ACS Omega
Online Access:http://dx.doi.org/10.1021/acsomega.7b00471