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Page 1
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.
Young JR, Huang SX, Walsh TF, Wyvratt MJ, Yang YT, Yudkovitz JB, Cui J, Mount GR, Ren RN, Wu TJ, Shen X, Lyons KA, Mao AH, Carlin JR, Karanam BV, Vincent SH, Cheng K, Goulet MT. Young JR, et al. Among authors: vincent sh. Bioorg Med Chem Lett. 2002 Mar 11;12(5):827-32. doi: 10.1016/s0960-894x(02)00026-4. Bioorg Med Chem Lett. 2002. PMID: 11859012
Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.
Simeone JP, Bugianesi RL, Ponpipom MM, Yang YT, Lo JL, Yudkovitz JB, Cui J, Mount GR, Ren RN, Creighton M, Mao AH, Vincent SH, Cheng K, Goulet MT. Simeone JP, et al. Among authors: vincent sh. Bioorg Med Chem Lett. 2002 Nov 18;12(22):3329-32. doi: 10.1016/s0960-894x(02)00751-5. Bioorg Med Chem Lett. 2002. PMID: 12392744
A potent, nonpeptidyl 1H-quinolone antagonist for the gonadotropin-releasing hormone receptor.
DeVita RJ, Walsh TF, Young JR, Jiang J, Ujjainwalla F, Toupence RB, Parikh M, Huang SX, Fair JA, Goulet MT, Wyvratt MJ, Lo JL, Ren N, Yudkovitz JB, Yang YT, Cheng K, Cui J, Mount G, Rohrer SP, Schaeffer JM, Rhodes L, Drisko JE, McGowan E, MacIntyre DE, Vincent S, Carlin JR, Cameron J, Smith RG. DeVita RJ, et al. J Med Chem. 2001 Mar 15;44(6):917-22. doi: 10.1021/jm000275p. J Med Chem. 2001. PMID: 11300873
Orally bioavailable, indole-based nonpeptide GnRH receptor antagonists with high potency and functional activity.
Ashton WT, Sisco RM, Kieczykowski GR, Yang YT, Yudkovitz JB, Cui J, Mount GR, Ren RN, Wu TJ, Shen X, Lyons KA, Mao AH, Carlin JR, Karanam BV, Vincent SH, Cheng K, Goulet MT. Ashton WT, et al. Among authors: vincent sh. Bioorg Med Chem Lett. 2001 Oct 8;11(19):2597-602. doi: 10.1016/s0960-894x(01)00512-1. Bioorg Med Chem Lett. 2001. PMID: 11551758
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.
Lin LS, Kopka IE, Mumford RA, Magriotis PA, Lanza T Jr, Durette PL, Kamenecka T, Young DN, de Laszlo SE, McCauley E, Riper GV, Kidambi U, Egger LA, Tong X, Lyons K, Vincent S, Stearns R, Colletti A, Teffera Y, Fenyk-Melody J, Schmidt JA, MacCoss M, Hagmann WK. Lin LS, et al. Bioorg Med Chem Lett. 2002 Feb 25;12(4):611-4. doi: 10.1016/s0960-894x(01)00818-6. Bioorg Med Chem Lett. 2002. PMID: 11844683
Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.
Kopka IE, Young DN, Lin LS, Mumford RA, Magriotis PA, MacCoss M, Mills SG, Van Riper G, McCauley E, Egger LE, Kidambi U, Schmidt JA, Lyons K, Stearns R, Vincent S, Colletti A, Wang Z, Tong S, Wang J, Zheng S, Owens K, Levorse D, Hagmann WK. Kopka IE, et al. Bioorg Med Chem Lett. 2002 Feb 25;12(4):637-40. doi: 10.1016/s0960-894x(01)00821-6. Bioorg Med Chem Lett. 2002. PMID: 11844689
Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.
Kopka IE, Lin LS, Mumford RA, Lanza T Jr, Magriotis PA, Young D, DeLaszlo SE, MacCoss M, Mills SG, Van Riper G, McCauley E, Lyons K, Vincent S, Egger LA, Kidambi U, Stearns R, Colletti A, Teffera Y, Tong S, Owens K, Levorse D, Schmidt JA, Hagmann WK. Kopka IE, et al. Bioorg Med Chem Lett. 2002 Sep 2;12(17):2415-8. doi: 10.1016/s0960-894x(02)00460-2. Bioorg Med Chem Lett. 2002. PMID: 12161146
Highly constrained bicyclic VLA-4 antagonists.
Chang LL, Truong Q, Doss GA, MacCoss M, Lyons K, McCauley E, Mumford R, Forrest G, Vincent S, Schmidt JA, Hagmann WK. Chang LL, et al. Bioorg Med Chem Lett. 2007 Feb 1;17(3):597-601. doi: 10.1016/j.bmcl.2006.11.011. Epub 2006 Nov 7. Bioorg Med Chem Lett. 2007. PMID: 17118652
The discovery of sulfonylated dipeptides as potent VLA-4 antagonists.
Hagmann WK, Durette PL, Lanza T, Kevin NJ, de Laszlo SE, Kopka IE, Young D, Magriotis PA, Li B, Lin LS, Yang G, Kamenecka T, Chang LL, Wilson J, MacCoss M, Mills SG, Van Riper G, McCauley E, Egger LA, Kidambi U, Lyons K, Vincent S, Stearns R, Colletti A, Teffera J, Tong S, Fenyk-Melody J, Owens K, Levorse D, Kim P, Schmidt JA, Mumford RA. Hagmann WK, et al. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2709-13. doi: 10.1016/s0960-894x(01)00544-3. Bioorg Med Chem Lett. 2001. PMID: 11591507
81 results