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Bioorg Med Chem Lett. 2012 Jan 1;22(1):733-7. doi: 10.1016/j.bmcl.2011.10.030. Epub 2011 Oct 14.

Indole RSK inhibitors. Part 1: discovery and initial SAR.

Author information

1
Department of Medicinal Chemistry, Boehringer-Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877, United States. stephen.boyer.b@gmail.com

Abstract

A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were identified through high throughput screening. An RSK crystal structure and exploratory SAR were used to define the series pharmacophore. Compounds with good cell potency, such as compounds 43, 44, and 55 were identified, and form the basis for subsequent kinase selectivity optimization.

PMID:
22100312
DOI:
10.1016/j.bmcl.2011.10.030
[Indexed for MEDLINE]

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