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Literature DB >> 18990570

Chroman-3-amides as potent Rho kinase inhibitors.

Yen Ting Chen¹, Thomas D Bannister, Amiee Weiser, Evelyn Griffin, Li Lin, Claudia Ruiz, Michael D Cameron, Stephan Schürer, Derek Duckett, Thomas Schröter, Philip LoGrasso, Yangbo Feng.

Abstract

Inhibition of Rho kinase (ROCK) is an attractive strategy for the treatment of diseases such as hypertension, glaucoma, and cancer. Here we report chroman-3-amides as highly potent ROCK inhibitors with sufficient kinase selectivity, excellent cell activity, good microsomal stability, and desirable pharmacokinetic properties for study as potential therapeutic agents.

Entities: Chemical Disease

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Year: 2008 PMID： 18990570 DOI： 10.1016/j.bmcl.2008.10.080

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

14 in total

Review 1. Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.

Authors: Rebecca K Donegan; Raquel L Lieberman
Journal: J Med Chem Date: 2015-09-25 Impact factor: 7.446

Review 2. Rho-kinase inhibitors as therapeutics: from pan inhibition to isoform selectivity.

Authors: C Hahmann; T Schroeter
Journal: Cell Mol Life Sci Date: 2009-11-12 Impact factor: 9.261

3. In silico prediction of ROCK II inhibitors by different classification approaches.

Authors: Chuipu Cai; Qihui Wu; Yunxia Luo; Huili Ma; Jiangang Shen; Yongbin Zhang; Lei Yang; Yunbo Chen; Zehuai Wen; Qi Wang
Journal: Mol Divers Date: 2017-08-02 Impact factor: 2.943

4. Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.

Authors: Yan Yin; Ke Zheng; Nibal Eid; Shannon Howard; Ji-Hak Jeong; Fei Yi; Jia Guo; Chul Min Park; Mathieu Bibian; Weilin Wu; Pamela Hernandez; HaJeung Park; Yuntao Wu; Jun-Li Luo; Philip V LoGrasso; Yangbo Feng
Journal: J Med Chem Date: 2015-02-04 Impact factor: 7.446

Chroman-3-amides as potent Rho kinase inhibitors.

Review 1. Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.

Review 2. Rho-kinase inhibitors as therapeutics: from pan inhibition to isoform selectivity.

3. In silico prediction of ROCK II inhibitors by different classification approaches.

4. Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.

5. Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).

Review 6. Potential benefits of rho-kinase inhibition in arterial hypertension.

7. A small molecule bidentate-binding dual inhibitor probe of the LRRK2 and JNK kinases.

8. ROCKing Regeneration: Rho Kinase Inhibition as Molecular Target for Neurorestoration.

9. Identification of potential small molecule binding pockets on Rho family GTPases.

10. Computer-aided discovery of phenylpyrazole based amides as potent S6K1 inhibitors.