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The Immunosuppressive Metabolite of Leflunomide Is a Potent Inhibitor of Human Dihydroorotate Dehydrogenase

✍ Scribed by Davis, June P.; Cain, Gary A.; Pitts, William J.; Magolda, Ronald L.; Copeland, Robert A.

Book ID
121345075
Publisher
American Chemical Society
Year
1996
Tongue
English
Weight
330 KB
Volume
35
Category
Article
ISSN
0006-2960

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The Ͱ-cyano-ͱ-hydroxy enamide 1 is an inhibitor of human dihydroorotate dehydrogenase (IC 50 ϭ 0.26 ȐM), the rate-limiting enzyme in the de novo pyrimidine biosynthesis. A structure-activity analysis based on selected derivatives of 1 demonstrates that both its structural characteristics and its phy