Design, synthesis and SAR of substituted indoles as selective TrkA inhibitors.

Authors: Hurzy DM1, Henze DA2, Cabalu TD3, Narayan K4, Heller A5, Cooke AJ6.
Publisher/Year: Bioorg Med Chem Lett. 2017 Jun 15; 27 (12): 2695-2701.
Pub Med ID/Journal ID: PMID: 28465100


A series of substituted indoles were examined as selective inhibitors of tropomyosin-related kinase receptor A (TrkA), a therapeutic target for the treatment of pain. An SAR optimization campaign based on ALIS screening lead compound 1 is reported.