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Molecules 2012, 17(2), 1373-1387;

Design, Synthesis and Anti-fibrosis Activity Study of N1-Substituted Phenylhydroquinolinone Derivatives

Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Central South University, Changsha 410013, Hunan, China
Division of Nephrology, Xiangya Hospital, Central South University, Changsha 410008, Hunan, China
Author to whom correspondence should be addressed.
Received: 27 December 2011 / Revised: 20 January 2012 / Accepted: 21 January 2012 / Published: 2 February 2012
(This article belongs to the Section Medicinal Chemistry)
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Pirfenidone (5-methyl-1-phenyl-2(1H)-pyridone, PFD) is a small-molecule compound acting on multiple targets involved in pathological fibrogenesis and is effective to increase the survival of patients with fibrosis, such as idiopathic pulmonary fibrosis. However, PFD is not active enough, requiring a high daily dose. In this study, to keep the multiple target profiles, N1-substituted phenylhydroquinolinone derivatives, which retain the 1-phenyl-2(1H)-pyridone scaffold were designed and synthesized. The preliminary anti-fibrosis activities for all target compounds were evaluated on a NIH3T3 fibroblast cell line using MTT assay methods. Most compounds showed significant inhibition on NIH3T3 cell proliferation with a IC50 range of 0.09–26 mM, among which 5-hydroxy-1-(4'-bromophenyl)-5,6,7,8-tetrahydroquinolin-2(1H)-one (6j) displayed 13 times higher potency (IC50 = 0.3 mM) than that of AKF-PD (IC50 = 4.2 mM). These results suggest that N1-substituted phenylhydroquinolinone is a promising scaffold which can be applied for further investigation and for developing novel anti-fibrosis agents. View Full-Text
Keywords: N1-substituted phenylhydroquinolinones; synthesis; anti-fibrosis N1-substituted phenylhydroquinolinones; synthesis; anti-fibrosis

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Wu, L.; Liu, B.; Li, Q.; Chen, J.; Tao, L.; Hu, G. Design, Synthesis and Anti-fibrosis Activity Study of N1-Substituted Phenylhydroquinolinone Derivatives. Molecules 2012, 17, 1373-1387.

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