Format

Send to:

Choose Destination
See comment in PubMed Commons below
Bioorg Med Chem Lett. 2012 Jan 1;22(1):738-42. doi: 10.1016/j.bmcl.2011.10.029. Epub 2011 Oct 18.

Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.

Author information

  • 1Department of Medicinal Chemistry, Boehringer-Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Road, PO Box 368, Ridgefield, CT 06877, USA. tom.kirrane@boehringer-ingelheim.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 optimized for cellular potency and kinase selectivity. This led to the identification of compound 24, BIX 02565, an attractive candidate for use in vitro and in vivo to explore the role of RSK as a target for the treatment heart failure.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
22056746
[PubMed - indexed for MEDLINE]

LinkOut - more resources

Full Text Sources

Other Literature Sources

Chemical Information

Molecular Biology Databases

PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Write to the Help Desk