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

Peter Lin, Mamta Parikh, Jane Ling Lo, Yi Tien Yang, Kang Cheng, Roy G. Smith, Michael H. Fisher, Matthew J. Wyvratt, Mark T. Goulet

Research output: Contribution to journalArticle

22 Scopus citations

Abstract

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.

Original languageEnglish (US)
Pages (from-to)1077-1080
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number8
DOIs
StatePublished - Apr 23 2001
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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  • Cite this

    Lin, P., Parikh, M., Lo, J. L., Yang, Y. T., Cheng, K., Smith, R. G., Fisher, M. H., Wyvratt, M. J., & Goulet, M. T. (2001). Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists. Bioorganic and Medicinal Chemistry Letters, 11(8), 1077-1080. https://doi.org/10.1016/S0960-894X(01)00133-0