Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors

Yen Ting Chen; Tomas Vojkovsky; Xingang Fang; Jennifer R. Pocas; Wayne Grant; Amiee M. W. Handy; Thomas Schröter; Philip LoGrasso; Thomas D. Bannister; Yangbo Feng

doi:10.1039/C0MD00194E

Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors†

Yen Ting Chen,^a Tomas Vojkovsky,^a Xingang Fang,^a Jennifer R. Pocas,^a Wayne Grant,^a Amiee M. W. Handy,^a Thomas Schröter,^a Philip LoGrasso,^a Thomas D. Bannister*^a and Yangbo Feng*^a

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^a Translational Research Institute, Scripps Florida, 130 Scripps Way #2A1, Jupiter, FL, USA
E-mail: tbannist@scripps.edu, yfeng@scripps.edu
Fax: +1-561-228-3089
Tel: +1 561 228 2201

Abstract

Rho kinase (ROCK) is currently investigated as a target for various diseases such as glaucoma and spinal cord injury. Herein, we report the asymmetric synthesis of chroman 1, a highly potent ROCK inhibitor, and its analogs. The inhibitory properties of these compounds for ROCK-II and a selected set of highly homologous kinases are also discussed.

MedChemComm

Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors†

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Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors

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