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. 2021 Feb 1:33:127721.
doi: 10.1016/j.bmcl.2020.127721. Epub 2020 Nov 28.

ROCK inhibitors 4: Structure-activity relationship studies of 7-azaindole-based rho kinase (ROCK) inhibitors

Upul K Bandarage  1 , John Court  2 , Huai Gao  2 , Suganthini Nanthakumar  2 , Jon H Come  2 , Simon Giroux  2 , Jeremy Green  2
Affiliations

ROCK inhibitors 4: Structure-activity relationship studies of 7-azaindole-based rho kinase (ROCK) inhibitors

Upul K Bandarage et al. Bioorg Med Chem Lett. .

Abstract

Rho kinase (ROCK) inhibitors are of therapeutic value for the treatment of disorders such as hypertension and glaucoma, and potentially of wider use against diseases such as cancer and multiple sclerosis. We previously reported a series of potent and selective ROCK inhibitors based on a substituted 7-azaindole scaffold. Here we extend the SAR exploration of the 7-azaindole series to identify leads for further evaluation. New compounds such as 16, 17, 19, 21 and 22 showed excellent ROCK potency and protein kinase A (PKA) selectivity, combined with microsome and hepatocyte stability.

Keywords: 7-Azaindole; Rho kinase (ROCK); Thiazole; protein kinase A (PKA).

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