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 Citations (Scopus)

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

Fingerprint

LHRH Receptors
Derivatives
Gonadotropin-Releasing Hormone
Inhibitory Concentration 50
Rats
Assays
Carbon
2-(3,5-dimethylphenyl)tryptamine

ASJC Scopus subject areas

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

Cite this

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 journalArticle

Lin, P, Parikh, M, Lo, JL, Yang, YT, Cheng, K, Smith, RG, Fisher, MH, Wyvratt, MJ & Goulet, MT 2001, 'Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists', Bioorganic and Medicinal Chemistry Letters, vol. 11, no. 8, pp. 1077-1080. https://doi.org/10.1016/S0960-894X(01)00133-0
Lin, Peter ; Parikh, Mamta ; Lo, Jane Ling ; Yang, Yi Tien ; Cheng, Kang ; Smith, Roy G. ; Fisher, Michael H. ; Wyvratt, Matthew J. ; Goulet, Mark T. / Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists. In: Bioorganic and Medicinal Chemistry Letters. 2001 ; Vol. 11, No. 8. pp. 1077-1080.
@article{8d32ce30da0e499aa67fd3127c454112,
title = "Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists",
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.",
author = "Peter Lin and Mamta Parikh and Lo, {Jane Ling} and Yang, {Yi Tien} and Kang Cheng and Smith, {Roy G.} and Fisher, {Michael H.} and Wyvratt, {Matthew J.} and Goulet, {Mark T.}",
year = "2001",
month = "4",
day = "23",
doi = "10.1016/S0960-894X(01)00133-0",
language = "English (US)",
volume = "11",
pages = "1077--1080",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "8",

}

TY - JOUR

T1 - Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists

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.

PY - 2001/4/23

Y1 - 2001/4/23

N2 - 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.

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.

UR - http://www.scopus.com/inward/record.url?scp=0035938412&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0035938412&partnerID=8YFLogxK

U2 - 10.1016/S0960-894X(01)00133-0

DO - 10.1016/S0960-894X(01)00133-0

M3 - Article

C2 - 11327594

AN - SCOPUS:0035938412

VL - 11

SP - 1077

EP - 1080

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 8

ER -