Document Report Card

Basic Information

ID: ALA4043256

Journal: Bioorg Med Chem Lett

Title: Discovery of N-substituted 7-azaindoles as PIM1 kinase inhibitors - Part I.

Authors: Barberis C, Moorcroft N, Arendt C, Levit M, Moreno-Mazza S, Batchelor J, Mechin I, Majid T.

Abstract: Novel N-substituted azaindoles have been discovered as PIM1 inhibitors. X-ray structures have played a significant role in orienting the chemistry effort in the initial phase of hit confirmation. Disclosure of an unconventional binding mode for 1 and 2, as demonstrated by X-ray crystallography, is presented and was an important factor in selecting and advancing a lead series.

CiteXplore: 28947155

DOI: 10.1016/j.bmcl.2017.08.069