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- Title
Structural Optimization and Structure–Activity Relationship of 4-Thiazolidinone Derivatives as Novel Inhibitors of Human Dihydroorotate Dehydrogenase.
- Authors
Zeng, Fanxun; Quan, Lina; Yang, Guantian; Qi, Tiantian; Zhang, Letian; Li, Shiliang; Li, Honglin; Zhu, Lili; Xu, Xiaoyong
- Abstract
Human dihydroorotate dehydrogenase (hDHODH), one of the attractive targets for the development of immunosuppressive drugs, is also a potential target of anticancer drugs and anti-leukemic drugs. The development of promising hDHODH inhibitors is in high demand. Based on the unique binding mode of our previous reported 4-thiazolidinone derivatives, via molecular docking method, three new series 4-thiazolidinone derivatives were designed and synthesized as hDHODH inhibitors. The preliminary structure–activity relationship was investigated. Compound 9 of biphenyl series and compound 37 of amide series displayed IC50 values of 1.32 μM and 1.45 μM, respectively. This research will provide valuable reference for the research of new structures of hDHODH inhibitors.
- Subjects
DIHYDROOROTATE dehydrogenase; STRUCTURE-activity relationships; STRUCTURAL optimization; IMMUNOSUPPRESSIVE agents; MOLECULAR docking; BIPHENYL compounds
- Publication
Molecules, 2019, Vol 24, Issue 15, p2780
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules24152780