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. 2010 Jun 1;20(11):3235-9.
doi: 10.1016/j.bmcl.2010.04.070. Epub 2010 Apr 22.

Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account

Frank Wu  1 , Frank H Büttner, Rhonda Chen, Eugene Hickey, Scott Jakes, Paul Kaplita, Mohammed A Kashem, Steven Kerr, Stanley Kugler, Zofia Paw, Anthony Prokopowicz, Cheng-Kon Shih, Roger Snow, Erick Young, Charles L Cywin
Affiliations

Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account

Frank Wu et al. Bioorg Med Chem Lett. .

Abstract

Two closely related scaffolds were identified through an uHTS campaign as desirable starting points for the development of Rho-Kinase (ROCK) inhibitors. Here, we describe our hit-to-lead evaluation process which culminated in the rapid discovery of potent leads such as 22 which successfully demonstrated an early in vivo proof of concept for anti-hypertensive activity.

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