2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain

JR Young, SX Huang, TF Walsh, MJ Wyvratt…

文献索引：Young, Jonathan R.; Huang, Song X.; Walsh, Thomas F.; Wyvratt Jr., Matthew J.; Yang, Yi Tien; Yudkovitz, Joel B.; Cui, Jisong; Mount, George R.; Ren, Rena Ning; Wu, Tsuei-Ju; Shen, Xiaolan; Lyons, Kathryn A.; Mao, An-Hua; Carlin, Josephine R.; Karanam, Bindhu V.; Vincent, Stella H.; Cheng, Kang; Goulet, Mark T. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 5 p. 827 - 832

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被引用次数: 40

摘要

A series of 2-arylindoles containing novel heteroaromatic substituents on the tryptamine tether, based on compound 1, was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. Successful modifications of 1 included chain length variation (reduction) and replacement of the pyridine with heteroaromatic groups. These alterations culminated in the discovery of compound 27kk ...