Bioorganic and Medicinal Chemistry Letters
Bioorganic and Medicinal Chemistry Letters
5 years ago

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

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

Publisher URL: www.sciencedirect.com/science

DOI: S0960894X17308703

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