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

doi:10.1016/S0960-894X(01)00133-0

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 journal › Article › peer-review

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 language	English (US)
Pages (from-to)	1077-1080
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	8
DOIs	https://doi.org/10.1016/S0960-894X(01)00133-0
State	Published - Apr 23 2001
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Biology
Organic Chemistry
Drug Discovery
Pharmaceutical Science

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Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists. / Lin, Peter; Parikh, Mamta; Lo, Jane Ling; Yang, Yi Tien; Cheng, Kang; Smith, Roy G.; Fisher, Michael H.; Wyvratt, Matthew J.; Goulet, Mark T.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 8, 23.04.2001, p. 1077-1080.

Research output: Contribution to journal › Article › peer-review

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AU - Lin, Peter

AU - Parikh, Mamta

AU - Lo, Jane Ling

AU - Yang, Yi Tien

AU - Cheng, Kang

AU - Smith, Roy G.

AU - Fisher, Michael H.

AU - Wyvratt, Matthew J.

AU - Goulet, Mark T.

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AB - 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.

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

Abstract

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