Author/Authors :
Peter Lin، نويسنده , , Mamta Parikh، نويسنده , , Jane-Ling Lo، نويسنده , , Yi Tien Yang، نويسنده , , Kang Cheng، نويسنده , , Roy G. Smith، نويسنده , , Michael H. Fisher، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Mark T. Goulet، نويسنده ,
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 16 nM.