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Updated: Jun 29, 2026

Enhancing the Engraftment of Human Induced Pluripotent Stem Cell-derived Cardiomyocytes via a Transient Inhibition of Rho Kinase Activity
Published on: July 10, 2019
Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic
Clark A Sehon1, Gren Z Wang, Andrew Q Viet
1Departments of Medicinal Chemistry, Investigative Biology, Vascular Biology, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, USA. clark.a.sehon@gsk.com
Abstract:
Recent studies using known Rho-associated kinase isoform 1 (ROCK1) inhibitors along with cellular and molecular biology data have revealed a pivotal role of this enzyme in many aspects of cardiovascular function. Here we report a series of ROCK1 inhibitors which were originally derived from a dihydropyrimidinone core 1. Our efforts focused on the optimization of dihydropyrimidine 2, which resulted in the identification of a series of dihydropyrimidines with improved pharmacokinetics and P450 properties.
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