title: Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.
abstract: Based on lead compounds 2 and 3 a series of 3,5-disubstituted pyridines have been designed and evaluated for inhibition of AKT/PKB. Modifications at the 3 position of the pyridine ring led to a number of potent compounds with improved physical properties, resulting in the identification of 11g as a promising, orally active Akt inhibitor. The synthesis, structure-activity relationship studies, and pharmacokinetic data are presented in this paper.
authors: Cancer Research, Department R47S, AP10 Abbott Laboratories, 100 Abbott Park Rd, Abbott Park, IL 60064, USA. sheela.thomas@abbott.com
authors: Sheela A
authors: SA
authors: Thomas
authors: Tongmei
authors: T
authors: Li
authors: Keith W
authors: KW
authors: Woods
authors: Xiaohong
authors: X
authors: Song
authors: Garrick
authors: G
authors: Packard
authors: John P
authors: JP
authors: Fischer
authors: Robert B
authors: RB
authors: Diebold
authors: Xuesong
authors: X
authors: Liu
authors: Yan
authors: Y
authors: Shi
authors: Vered
authors: V
authors: Klinghofer
authors: Eric F
authors: EF
authors: Johnson
authors: Jennifer J
authors: JJ
authors: Bouska
authors: Amanda
authors: A
authors: Olson
authors: Ran
authors: R
authors: Guan
authors: Shayna R
authors: SR
authors: Magnone
authors: Kennan
authors: K
authors: Marsh
authors: Yan
authors: Y
authors: Luo
authors: Saul H
authors: SH
authors: Rosenberg
authors: Vincent L
authors: VL
authors: Giranda
authors: Qun
authors: Q
authors: Li