Synthesis and biological evaluation of piperazinyl heterocyclic antagonists of the gonadotropin releasing hormone (GnRH) receptor

…, DB Hauze, CW Mann, JF Mehlmann, JF Rogers…

Index: Vera, Matthew D.; Lundquist IV, Joseph T.; Chengalvala, Murty V.; Cottom, Joshua E.; Feingold, Irene B.; Garrick, Lloyd M.; Green, Daniel M.; Hauze, Diane B.; Mann, Charles W.; Mehlmann, John F.; Rogers, John F.; Shanno, Linda; Wrobel, Jay E.; Pelletier, Jeffrey C. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 8 p. 2512 - 2515

Full Text: HTML

Citation Number: 3

Abstract

Antagonism of the gonadotropin releasing hormone (GnRH) receptor has resulted in positive clinical results in reproductive tissue disorders such as endometriosis and prostate cancer. Following the recent discovery of orally active GnRH antagonists based on a 4- piperazinylbenzimidazole template, we sought to investigate the properties of heterocyclic isosteres of the benzimidazole template. We report here the synthesis and biological ...

Related Articles:

Synthesis of 4-[4'-(N, N-Dimethylsulfamoyl) piperazin-1-yl]-pyridine Derivatives as Sorbitol Dehydrogenase Porentioal Inhibitors

[Heterocycles, , vol. 53, # 4 p. 797 - 804]

Cytochrome P450-mediated biotransformation of sorafenib and its N-oxide metabolite: implications for cell viability and human toxicity

[Varlet, Didier; Fourmaintraux, Eric; Depreux, Patrick; Lesieur, Daniel Heterocycles, 2000 , vol. 53, # 4 p. 797 - 804]

Synthesis and Biological Evaluation of Novel 4??(2??Fluorophenoxy)??2??(1H??tetrazol??1??yl) pyridines Bearing Semicarbazone Moieties as Potent Antitumor Agents

[Archiv der Pharmazie, , vol. 346, # 11 p. 840 - 850]

Synthesis of 4-[4'-(N, N-Dimethylsulfamoyl) piperazin-1-yl]-pyridine Derivatives as Sorbitol Dehydrogenase Porentioal Inhibitors

[Heterocycles, , vol. 53, # 4 p. 797 - 804]

More Articles...