Author/Authors :
Jonathan R. Young، نويسنده , , Song X. Huang، نويسنده , , Thomas F. Walsh، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Yi Tien Yang، نويسنده , , Joel B. Yudkovitz، نويسنده , , Jisong Cui، نويسنده , , George R. Mount، نويسنده , , Rena Ning Ren، نويسنده , , Tsuei-Ju Wu، نويسنده , , Xiaolan Shen، نويسنده , , Kathryn A. Lyons، نويسنده , , Sheng-Hua Mao، نويسنده , , Josephine R. Carlin، نويسنده , , Bindhu V. Karanam، نويسنده , , Stella H. Vincent، نويسنده , , Kang Cheng، نويسنده , , Mark T. Goulet، نويسنده ,
Abstract :
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 which had excellent in vitro potency and oral efficacy in rodents.
