Heterocyclic derivatives of 2-(3, 5-dimethylphenyl) tryptamine as GnRH receptor antagonists

…, M Parikh, JL Lo, YT Yang, K Cheng, RG Smith…

文献索引：Lin, Peter; Parikh, Mamta; Lo, Jane-Ling; Yang, Yi Tien; Cheng, Kang; Smith, Roy G; Fisher, Michael H; Wyvratt, Matthew J; Goulet, Mark T Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 8 p. 1077 - 1080

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被引用次数: 23

摘要

A series of heterocyclic 2-(3, 5-dimethylphenyl) tryptamine derivatives was prepared and evaluated on a rat gonadotropin releasing hormone receptor assay. The carbon tether length and heterocyclic ring attached to the amino group of 2-(3, 5-dimethylphenyl) tryptamine were varied. Several of these derivatives were potent GnRH antagonists with the most potent compound having an IC50 of 16nM.