| Summary: | Human dihydroorotate dehydrogenase (<i>h</i>DHODH), 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 <i>h</i>DHODH 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 <i>h</i>DHODH inhibitors. The preliminary structure−activity relationship was investigated. Compound <b>9</b> of biphenyl series and compound <b>37</b> of amide series displayed IC<sub>50</sub> values of 1.32 μM and 1.45 μM, respectively. This research will provide valuable reference for the research of new structures of <i>h</i>DHODH inhibitors.
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