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Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
Hudkins RL, Raddatz R, Tao M, Mathiasen JR, Aimone LD, Becknell NC, Prouty CP, Knutsen LJ, Yazdanian M, Moachon G, Ator MA, Mallamo JP, Marino MJ, Bacon ER, Williams M. Hudkins RL, et al. Among authors: mallamo jp. J Med Chem. 2011 Jul 14;54(13):4781-92. doi: 10.1021/jm200401v. Epub 2011 Jun 2. J Med Chem. 2011. PMID: 21634396
A new class of potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: structure-activity relationships for a series of 9-alkoxymethyl-12-(3-hydroxypropyl)indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-ones and the identification of CEP-5214 and its dimethylglycine ester prodrug clinical candidate CEP-7055.
Gingrich DE, Reddy DR, Iqbal MA, Singh J, Aimone LD, Angeles TS, Albom M, Yang S, Ator MA, Meyer SL, Robinson C, Ruggeri BA, Dionne CA, Vaught JL, Mallamo JP, Hudkins RL. Gingrich DE, et al. Among authors: mallamo jp. J Med Chem. 2003 Dec 4;46(25):5375-88. doi: 10.1021/jm0301641. J Med Chem. 2003. PMID: 14640546
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.
Dorsey BD, Iqbal M, Chatterjee S, Menta E, Bernardini R, Bernareggi A, Cassarà PG, D'Arasmo G, Ferretti E, De Munari S, Oliva A, Pezzoni G, Allievi C, Strepponi I, Ruggeri B, Ator MA, Williams M, Mallamo JP. Dorsey BD, et al. Among authors: mallamo jp. J Med Chem. 2008 Feb 28;51(4):1068-72. doi: 10.1021/jm7010589. Epub 2008 Feb 5. J Med Chem. 2008. PMID: 18247547
Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
Hudkins RL, Diebold JL, Tao M, Josef KA, Park CH, Angeles TS, Aimone LD, Husten J, Ator MA, Meyer SL, Holskin BP, Durkin JT, Fedorov AA, Fedorov EV, Almo SC, Mathiasen JR, Bozyczko-Coyne D, Saporito MS, Scott RW, Mallamo JP. Hudkins RL, et al. Among authors: mallamo jp. J Med Chem. 2008 Sep 25;51(18):5680-9. doi: 10.1021/jm8005838. Epub 2008 Aug 21. J Med Chem. 2008. PMID: 18714982
CEP-26401 (irdabisant), a potent and selective histamine H₃ receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities.
Raddatz R, Hudkins RL, Mathiasen JR, Gruner JA, Flood DG, Aimone LD, Le S, Schaffhauser H, Duzic E, Gasior M, Bozyczko-Coyne D, Marino MJ, Ator MA, Bacon ER, Mallamo JP, Williams M. Raddatz R, et al. Among authors: mallamo jp. J Pharmacol Exp Ther. 2012 Jan;340(1):124-33. doi: 10.1124/jpet.111.186585. Epub 2011 Oct 14. J Pharmacol Exp Ther. 2012. PMID: 22001260
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K, Jones-Bolin S, Zhao H, Bacon ER, Mallamo JP, Ator MA, Ruggeri BA. Hudkins RL, et al. Among authors: mallamo jp. J Med Chem. 2012 Jan 26;55(2):903-13. doi: 10.1021/jm201449n. Epub 2012 Jan 6. J Med Chem. 2012. PMID: 22148921
Overview of drug discovery and development.
Ator MA, Mallamo JP, Williams M. Ator MA, et al. Among authors: mallamo jp. Curr Protoc Pharmacol. 2006 Dec;Chapter 9:Unit9.9. doi: 10.1002/0471141755.ph0909s35. Curr Protoc Pharmacol. 2006. PMID: 22294181
43 results