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

@article{Lin2001HeterocyclicDO,
  title={Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists.},
  author={P Lin and Mamta Parikh and J L Lo and Yi Yang and Kang Cheng and R. G. Smith and Michael H. Fisher and Matthew J. Wyvratt and Mark T. Goulet},
  journal={Bioorganic \& medicinal chemistry letters},
  year={2001},
  volume={11 8},
  pages={
          1077-80
        }
}
  • P. Lin, M. Parikh, +6 authors M. Goulet
  • Published 23 April 2001
  • Chemistry, Medicine
  • Bioorganic & medicinal chemistry letters
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 16 nM. 
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