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Page 1
Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
Xiao HY, Balog A, Attar RM, Fairfax D, Fleming LB, Holst CL, Martin GS, Rossiter LM, Chen J, Cvjic ME, Dell-John J, Geng J, Gottardis MM, Han WC, Nation A, Obermeier M, Rizzo CA, Schweizer L, Spires T Jr, Shan W, Gavai A, Salvati ME, Vite G. Xiao HY, et al. Among authors: gottardis mm. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4491-5. doi: 10.1016/j.bmcl.2010.06.034. Epub 2010 Jun 10. Bioorg Med Chem Lett. 2010. PMID: 20584610
Pyrrolo[1,2-f]triazines as JAK2 inhibitors: achieving potency and selectivity for JAK2 over JAK3.
Harikrishnan LS, Kamau MG, Wan H, Inghrim JA, Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Lombardo LJ, Poss MA, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Baldwin KF, Lippy J, Nirschl DS, Qiu R, Miller AV, Khan J, Sack JS, Purandare AV. Harikrishnan LS, et al. Among authors: gottardis mm. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1425-8. doi: 10.1016/j.bmcl.2011.01.022. Epub 2011 Jan 11. Bioorg Med Chem Lett. 2011. PMID: 21282055
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.
Zimmermann K, Sang X, Mastalerz HA, Johnson WL, Zhang G, Liu Q, Batt D, Lombardo LJ, Vyas D, Trainor GL, Tokarski JS, Lorenzi MV, You D, Gottardis MM, Lippy J, Khan J, Sack JS, Purandare AV. Zimmermann K, et al. Among authors: gottardis mm. Bioorg Med Chem Lett. 2015 Jul 15;25(14):2809-12. doi: 10.1016/j.bmcl.2015.04.101. Epub 2015 May 11. Bioorg Med Chem Lett. 2015. PMID: 25987372
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.
Salvati ME, Balog A, Shan W, Rampulla R, Giese S, Mitt T, Furch JA, Vite GD, Attar RM, Jure-Kunkel M, Geng J, Rizzo CA, Gottardis MM, Krystek SR, Gougoutas J, Galella MA, Obermeier M, Fura A, Chandrasena G. Salvati ME, et al. Among authors: gottardis mm. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1910-5. doi: 10.1016/j.bmcl.2008.02.006. Epub 2008 Feb 8. Bioorg Med Chem Lett. 2008. PMID: 18291644
The discovery of BMS-737 as a potent, CYP17 lyase-selective inhibitor for the treatment of castration-resistant prostate cancer.
Padmakar Darne C, Velaparthi U, Saulnier M, Frennesson D, Liu P, Huang A, Tokarski J, Fura A, Spires T, Newitt J, Spires VM, Obermeier MT, Elzinga PA, Gottardis MM, Jayaraman L, Vite GD, Balog A. Padmakar Darne C, et al. Among authors: gottardis mm. Bioorg Med Chem Lett. 2022 Nov 1;75:128951. doi: 10.1016/j.bmcl.2022.128951. Epub 2022 Aug 27. Bioorg Med Chem Lett. 2022. PMID: 36031020
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