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Page 1
Synthesis and structure-activity relationship of imidazo(1,2-a)thieno(3,2-e)pyrazines as IKK-beta inhibitors.
Belema M, Bunker A, Nguyen VN, Beaulieu F, Ouellet C, Qiu Y, Zhang Y, Martel A, Burke JR, McIntyre KW, Pattoli MA, Daloisio C, Gillooly KM, Clarke WJ, Brassil PJ, Zusi FC, Vyas DM. Belema M, et al. Among authors: clarke wj. Bioorg Med Chem Lett. 2007 Aug 1;17(15):4284-9. doi: 10.1016/j.bmcl.2007.05.031. Epub 2007 May 16. Bioorg Med Chem Lett. 2007. PMID: 17540562
Design and synthesis of a fluoroindolocarbazole series as selective topoisomerase I active agents. Discovery of water-soluble 3,9-difluoro-12,13-dihydro-13-[6-amino-beta-D-glucopyranosyl]-5H,13H-benzo[b]- thienyl[2,3-a]pyrrolo[3,4-c]carbazole- 5,7(6H)-dione (BMS-251873) with curative antitumor activity against prostate carcinoma xenograft tumor model.
Balasubramanian BN, St Laurent DR, Saulnier MG, Long BH, Bachand C, Beaulieu F, Clarke W, Deshpande M, Eummer J, Fairchild CR, Frennesson DB, Kramer R, Lee FY, Mahler M, Martel A, Naidu BN, Rose WC, Russell J, Ruediger E, Solomon C, Stoffan KM, Wong H, Wright JJ, Zimmermann K, Vyas DM. Balasubramanian BN, et al. J Med Chem. 2004 Mar 25;47(7):1609-12. doi: 10.1021/jm034197s. J Med Chem. 2004. PMID: 15027851
Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Wittman M, Carboni J, Attar R, Balasubramanian B, Balimane P, Brassil P, Beaulieu F, Chang C, Clarke W, Dell J, Eummer J, Frennesson D, Gottardis M, Greer A, Hansel S, Hurlburt W, Jacobson B, Krishnananthan S, Lee FY, Li A, Lin TA, Liu P, Ouellet C, Sang X, Saulnier MG, Stoffan K, Sun Y, Velaparthi U, Wong H, Yang Z, Zimmermann K, Zoeckler M, Vyas D. Wittman M, et al. J Med Chem. 2005 Sep 8;48(18):5639-43. doi: 10.1021/jm050392q. J Med Chem. 2005. PMID: 16134929
Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists.
Gillman KW, Higgins MA, Poindexter GS, Browning M, Clarke WJ, Flowers S, Grace JE Jr, Hogan JB, McGovern RT, Iben LG, Mattson GK, Ortiz A, Rassnick S, Russell JW, Antal-Zimanyi I. Gillman KW, et al. Among authors: clarke wj. Bioorg Med Chem. 2006 Aug 15;14(16):5517-26. doi: 10.1016/j.bmc.2006.04.042. Epub 2006 May 11. Bioorg Med Chem. 2006. PMID: 16697206
Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.
Velaparthi U, Wittman M, Liu P, Carboni JM, Lee FY, Attar R, Balimane P, Clarke W, Sinz MW, Hurlburt W, Patel K, Discenza L, Kim S, Gottardis M, Greer A, Li A, Saulnier M, Yang Z, Zimmermann K, Trainor G, Vyas D. Velaparthi U, et al. J Med Chem. 2008 Oct 9;51(19):5897-900. doi: 10.1021/jm800832q. Epub 2008 Sep 3. J Med Chem. 2008. PMID: 18763755
Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors: SAR of a series of 3-[6-(4-substituted-piperazin-1-yl)-4-methyl-1H-benzimidazol-2-yl]-1H-pyridine-2-one.
Velaparthi U, Saulnier MG, Wittman MD, Liu P, Frennesson DB, Zimmermann K, Carboni JM, Gottardis M, Li A, Greer A, Clarke W, Yang Z, Menard K, Lee FY, Trainor G, Vyas D. Velaparthi U, et al. Bioorg Med Chem Lett. 2010 May 15;20(10):3182-5. doi: 10.1016/j.bmcl.2010.03.057. Epub 2010 Mar 27. Bioorg Med Chem Lett. 2010. PMID: 20399649
Heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 receptor antagonist.
Luo G, Chen L, Hu S, Huang Y, Mattson G, Iben LG, Russell JW, Clarke WJ, Hogan JB, Antal-Zimanyi I, Poindexter GS. Luo G, et al. Among authors: clarke wj. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3814-7. doi: 10.1016/j.bmcl.2013.04.095. Epub 2013 May 15. Bioorg Med Chem Lett. 2013. PMID: 23726344
75 results