An article Discovery of a novel series of hDHODH inhibitors with anti-pulmonary fibrotic activities WOS:000464108100006 published article about HUMAN DIHYDROOROTATE DEHYDROGENASE; DRUG in [Lu, Kuan; Zhao, Yanfang; Wu, Guodong; Hu, Hao; Jiang, Yuyang] Shenyang Pharmaceut Univ, Dept Pharmaceut Engn, Shenyang 110016, Liaoning, Peoples R China; [Lu, Kuan; Wang, Mingzhong] Sherushen Kivita Innovat Drug Discovery Inst, Sherushen 518057, Peoples R China; [Jiang, Yuyang] Tsinghua Univ, Natl & Local United Engn Lab Personalised Antitum, Grad Sch Shenshen, Shenzhen 518055, Peoples R China; [Jiang, Yuyang] Tsinghua Univ, Dept Pharmacol & Pharmaceut Sci, Sch Med, Beijing 100084, Peoples R China; [Gong, Guowei] Zunyi Med Univ, Dept Bioengn, Zhuhai Campus, Zhuhai 519041, Guangdong, Peoples R China in 2019, Cited 17. The Name is 3-(Trifluoromethyl)phenol. Through research, I have a further understanding and discovery of 98-17-9. Recommanded Product: 98-17-9
Human dihydroorotate dehydrogenase (hDHODH) is a flavin-dependent enzyme essential to pyrimidine de novo biosynthesis, which serves as an attractive therapeutic target for the treatment of autoimmune disorders. A novel series of hDHODH inhibitors was developed based on a lead which was obtained by a medicinal chemistry exploration. Most compounds showed moderate to significant potency against hDHODH, compounds 5d, 5e, and 6a effectively inhibited the activities of hDHODH with IC50 values from 0.9 to 2.8 mu M. Further studies showed that compound 5e also effectively suppressed proliferation of the activated PBMCs (IC50 = 20.35 mu M). Surprisingly, compound 5e also showed anti-pulmonary fibrotic activity similar to that of pirfenidone in vitro assay. Therefore, compound 5e might have potential to be developed as a novel hDHODH inhibitors for auto-immune diseases therapy.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles