Issue 63, 2016
From the journal:

RSC Advances

Discovery of lipoic acid-4-phenyl-1H-pyrazole hybrids as novel bifunctional ROCK inhibitors with antioxidant activity†

Ya-lin Tu,abc   Qiu-he Chen,abc   Sheng-nan Wang,abc   Asko Uri,d   Xiao-hong Yang,abc   Jia-qi Chu,abc   Jing-kao Chen,abc   Bing-ling Luo,be   Xiao-hong Chen,f   Shi-jun Wen*be  and  Rong-biao Pi*abcg  

* Corresponding authors

a School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou 510006, China
E-mail: pirb@mail.sysu.edu.cn

b International Joint Laboratory (SYSU-PolyU HK) of Novel Anti-Dementia Drugs of Guangdong, Guangzhou 510006, China

c National and Local United Engineering Lab of Druggability and New Drugs Evaluation, Sun Yat-sen University, Guangzhou 510006, China

d Institute of Chemistry, University of Tartu, Ravila St., Tartu 50411, Estonia

e Sun Yat-sen University Cancer Center, State Key Laboratory of Oncology in South China, Collaborative Innovation Center for Cancer Medicine, 651 Dongfeng East Road, Guangzhou 510060, China

f Department of Neurology, The Third Affiliated Hospital, Sun Yat-Sen University, Guangzhou, China

g Guangdong Province Key Laboratory of Brain Function and Disease, Zhongshan School of Medicine, Sun Yat-sen University, Guangzhou, China

Abstract

A series of lipoic acid (LA) and 4-phenyl-1H-pyrazole hybrids as bifunctional Rho-associated kinase (ROCK) inhibitors were designed, synthesized and evaluated. Compound 15 is identified to be a novel potent bifunctional ROCK inhibitor with antioxidant activity and neuroprotection.

Graphical abstract: Discovery of lipoic acid-4-phenyl-1H-pyrazole hybrids as novel bifunctional ROCK inhibitors with antioxidant activity

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Article information

DOI
https://doi.org/10.1039/C6RA12081D
Article type
Communication
Submitted
10 May 2016
Accepted
04 Jun 2016
First published
13 Jun 2016

RSC Adv., 2016,6, 58516-58520

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Discovery of lipoic acid-4-phenyl-1H-pyrazole hybrids as novel bifunctional ROCK inhibitors with antioxidant activity

Y. Tu, Q. Chen, S. Wang, A. Uri, X. Yang, J. Chu, J. Chen, B. Luo, X. Chen, S. Wen and R. Pi, RSC Adv., 2016, 6, 58516 DOI: 10.1039/C6RA12081D

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