Rapid Assembly of Diverse and Potent Allosteric Akt Inhibitors

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2008 Feb 26

PMID 18296048

Citations 11

Authors

Zhicai Wu

Ronald G Robinson

Sheng Fu

Stanley F Barnett

Deborah Defeo-Jones

Raymond E Jones

Astrid M Kral

Hans E Huber

Nancy E Kohl

George D Hartman

Mark T Bilodeau

Affiliations

Soon will be listed here.

Abstract

This paper describes the rapid assembly of four different classes of potent Akt inhibitors from a common intermediate. Among them, a pyridopyrimidine series displayed the best intrinsic and cell potency against Akt1 and Akt2. This series also showed a promising pharmacokinetic profile and excellent selectivity over other closely related kinases.

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