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Page 1
Development of 2-(5,6,7-Trifluoro-1H-Indol-3-yl)-quinoline-5-carboxamide as a Potent, Selective, and Orally Available Inhibitor of Human Androgen Receptor Targeting Its Binding Function-3 for the Treatment of Castration-Resistant Prostate Cancer.
Leblanc E, Ban F, Cavga AD, Lawn S, Huang CF, Mohan S, Chang MEK, Flory MR, Ghaidi F, Lingadahalli S, Chen G, Yu IPL, Morin H, Lallous N, Gleave ME, Mohammed H, Young RN, Rennie PS, Lack NA, Cherkasov A. Leblanc E, et al. Among authors: young rn. J Med Chem. 2021 Oct 28;64(20):14968-14982. doi: 10.1021/acs.jmedchem.1c00681. Epub 2021 Oct 18. J Med Chem. 2021. PMID: 34661404
Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).
Sturino CF, O'Neill G, Lachance N, Boyd M, Berthelette C, Labelle M, Li L, Roy B, Scheigetz J, Tsou N, Aubin Y, Bateman KP, Chauret N, Day SH, Lévesque JF, Seto C, Silva JH, Trimble LA, Carriere MC, Denis D, Greig G, Kargman S, Lamontagne S, Mathieu MC, Sawyer N, Slipetz D, Abraham WM, Jones T, McAuliffe M, Piechuta H, Nicoll-Griffith DA, Wang Z, Zamboni R, Young RN, Metters KM. Sturino CF, et al. Among authors: young rn. J Med Chem. 2007 Feb 22;50(4):794-806. doi: 10.1021/jm0603668. J Med Chem. 2007. PMID: 17300164
The discovery of MK-0674, an orally bioavailable cathepsin K inhibitor.
Isabel E, Bateman KP, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Gauthier JY, Lamontagne S, Lau CK, Léger S, LeRiche T, Lévesque JF, Li CS, Massé F, McKay DJ, Mellon C, Nicoll-Griffith DA, Oballa RM, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Wesolowski G, Young RN, Zamboni R, Black WC. Isabel E, et al. Among authors: young rn. Bioorg Med Chem Lett. 2010 Feb 1;20(3):887-92. doi: 10.1016/j.bmcl.2009.12.083. Epub 2009 Dec 28. Bioorg Med Chem Lett. 2010. PMID: 20061146
Identification of pyruvate kinase in methicillin-resistant Staphylococcus aureus as a novel antimicrobial drug target.
Zoraghi R, See RH, Axerio-Cilies P, Kumar NS, Gong H, Moreau A, Hsing M, Kaur S, Swayze RD, Worrall L, Amandoron E, Lian T, Jackson L, Jiang J, Thorson L, Labriere C, Foster L, Brunham RC, McMaster WR, Finlay BB, Strynadka NC, Cherkasov A, Young RN, Reiner NE. Zoraghi R, et al. Among authors: young rn. Antimicrob Agents Chemother. 2011 May;55(5):2042-53. doi: 10.1128/AAC.01250-10. Epub 2011 Feb 28. Antimicrob Agents Chemother. 2011. PMID: 21357306 Free PMC article.
Cheminformatics-driven discovery of selective, nanomolar inhibitors for staphylococcal pyruvate kinase.
Axerio-Cilies P, See RH, Zoraghi R, Worral L, Lian T, Stoynov N, Jiang J, Kaur S, Jackson L, Gong H, Swayze R, Amandoron E, Kumar NS, Moreau A, Hsing M, Strynadka NC, McMaster WR, Finlay BB, Foster LJ, Young RN, Reiner NE, Cherkasov A. Axerio-Cilies P, et al. Among authors: young rn. ACS Chem Biol. 2012 Feb 17;7(2):350-9. doi: 10.1021/cb2003576. Epub 2011 Nov 21. ACS Chem Biol. 2012. PMID: 22066782
Optimization and structure-activity relationships of a series of potent inhibitors of methicillin-resistant Staphylococcus aureus (MRSA) pyruvate kinase as novel antimicrobial agents.
Kumar NS, Amandoron EA, Cherkasov A, Finlay BB, Gong H, Jackson L, Kaur S, Lian T, Moreau A, Labrière C, Reiner NE, See RH, Strynadka NC, Thorson L, Wong EW, Worrall L, Zoraghi R, Young RN. Kumar NS, et al. Among authors: young rn. Bioorg Med Chem. 2012 Dec 15;20(24):7069-82. doi: 10.1016/j.bmc.2012.10.002. Epub 2012 Oct 17. Bioorg Med Chem. 2012. PMID: 23141418
Discovery and optimization of a new class of pyruvate kinase inhibitors as potential therapeutics for the treatment of methicillin-resistant Staphylococcus aureus infections.
Kumar NS, Dullaghan EM, Finlay BB, Gong H, Reiner NE, Jon Paul Selvam J, Thorson LM, Campbell S, Vitko N, Richardson AR, Zoraghi R, Young RN. Kumar NS, et al. Among authors: young rn. Bioorg Med Chem. 2014 Mar 1;22(5):1708-25. doi: 10.1016/j.bmc.2014.01.020. Epub 2014 Jan 24. Bioorg Med Chem. 2014. PMID: 24508307 Free PMC article.
Identification of a potent antiandrogen that targets the BF3 site of the androgen receptor and inhibits enzalutamide-resistant prostate cancer.
Munuganti RS, Hassona MD, Leblanc E, Frewin K, Singh K, Ma D, Ban F, Hsing M, Adomat H, Lallous N, Andre C, Jonadass JP, Zoubeidi A, Young RN, Guns ET, Rennie PS, Cherkasov A. Munuganti RS, et al. Among authors: young rn. Chem Biol. 2014 Nov 20;21(11):1476-85. doi: 10.1016/j.chembiol.2014.09.012. Chem Biol. 2014. PMID: 25459660
92 results