Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors

Yan Yin; Li Lin; Claudia Ruiz; Michael D Cameron; Jennifer Pocas; Wayne Grant; Thomas Schröter; Weimin Chen; Derek Duckett; Stephan Schürer; Philip LoGrasso; Yangbo Feng

doi:10.1016/j.bmcl.2009.09.115

Back

Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors

Journal article

Peer reviewed

Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors

Yan Yin, Li Lin, Claudia Ruiz, Michael D Cameron, Jennifer Pocas, Wayne Grant, Thomas Schröter, Weimin Chen, Derek Duckett, Stephan Schürer, …

Bioorganic & medicinal chemistry letters, Vol.19(23), pp.6686-6690

2009

DOI: https://doi.org/10.1016/j.bmcl.2009.09.115

PMID: 19837589

Abstract

Glaucoma

Rho

ROCK

Chroman

Benzothiazole

Pyrazole

ROCK inhibitors have been developed from 2-chromanyl- and 2-carboxamido-benzothiazoles. SAR studies and lead optimizations are described, which result in novel ROCK-II inhibitors with sub-nanomolar IC 50s and good kinase selectivity. A series of benzothiazole derivatives as ROCK inhibitors have been discovered. Compounds with good biochemical and cellular potency, and sufficient kinase selectivity have been identified.

Metrics

13 Record Views

40 Times Cited - Web of Science

See more details

InCites Highlights

These are selected metrics from InCites Benchmarking & Analytics tool, related to this output

Collaboration types: Domestic collaboration
Citation topics: 1 Clinical & Life Sciences; 1.96 Cell Biology; 1.96.224 Integrins
Web Of Science research areas: Chemistry, Medicinal; Chemistry, Organic
ESI research areas: Chemistry

UN Sustainable Development Goals (SDGs)

This output has contributed to the advancement of the following goals:

Source: InCites

Details

Title: Benzothiazoles as Rho-associated kinase (ROCK-II) inhibitors
Creators: Yan Yin - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Li Lin - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Claudia Ruiz - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Michael D Cameron - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Jennifer Pocas - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Wayne Grant - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Thomas Schröter - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Weimin Chen - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Derek Duckett - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Stephan Schürer - Department of Pharmacology and Center for Computational Science, University of Miami, Miami, FL 33136, United States
Philip LoGrasso - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Yangbo Feng - Translational Research Institute and Department of Molecular Therapeutics, The Scripps Research Institute, Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, United States
Publication Details: Bioorganic & medicinal chemistry letters, Vol.19(23), pp.6686-6690
Publisher: Elsevier Ltd
Academic Unit: Miller School of Medicine; Molecular and Cellular Pharmacology Research
Language: English
Resource Type: Journal article
PMID: 19837589
Record Identifier: 991031560786002976