Chroman-3-amides As Potent Rho Kinase Inhibitors

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2008 Nov 8

PMID 18990570

Citations 15

Authors

Yen Ting Chen

Thomas D Bannister

Amiee Weiser

Evelyn Griffin

Li Lin

Claudia Ruiz

Michael D Cameron

Stephan Schurer

Derek Duckett

Thomas Schroter

Philip LoGrasso

Yangbo Feng

Affiliations

Soon will be listed here.

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.

Citing Articles

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

Yin Y, Sun Y, Zhao L, Pan J, Feng Y RSC Med Chem. 2021; 11(5):583-590.

PMID: 33479660 PMC: 7605259. DOI: 10.1039/c9md00537d.

ROCK inhibitors upregulate the neuroprotective Parkin-mediated mitophagy pathway.

Moskal N, Riccio V, Bashkurov M, Taddese R, Datti A, Lewis P Nat Commun. 2020; 11(1):88.

PMID: 31900402 PMC: 6941965. DOI: 10.1038/s41467-019-13781-3.

Mutant huntingtin enhances activation of dendritic Kv4 K channels in striatal spiny projection neurons.

Carrillo-Reid L, Day M, Xie Z, Melendez A, Kondapalli J, Plotkin J Elife. 2019; 8.

PMID: 31017573 PMC: 6481990. DOI: 10.7554/eLife.40818.

Discovery of Novel N-Substituted Prolinamido Indazoles as Potent Rho Kinase Inhibitors and Vasorelaxation Agents.

Yao Y, Li R, Liu X, Yang F, Yang Y, Li X Molecules. 2017; 22(10).

PMID: 29048389 PMC: 6151428. DOI: 10.3390/molecules22101766.

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

Cai C, Wu Q, Luo Y, Ma H, Shen J, Zhang Y Mol Divers. 2017; 21(4):791-807.

PMID: 28770474 DOI: 10.1007/s11030-017-9772-5.