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Page 1
Identification of dipeptidyl nitriles as potent and selective inhibitors of cathepsin B through structure-based drug design.
Greenspan PD, Clark KL, Tommasi RA, Cowen SD, McQuire LW, Farley DL, van Duzer JH, Goldberg RL, Zhou H, Du Z, Fitt JJ, Coppa DE, Fang Z, Macchia W, Zhu L, Capparelli MP, Goldstein R, Wigg AM, Doughty JR, Bohacek RS, Knap AK. Greenspan PD, et al. Among authors: tommasi ra. J Med Chem. 2001 Dec 20;44(26):4524-34. doi: 10.1021/jm010206q. J Med Chem. 2001. PMID: 11741472
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.
Greenspan PD, Clark KL, Cowen SD, McQuire LW, Tommasi RA, Farley DL, Quadros E, Coppa DE, Du Z, Fang Z, Zhou H, Doughty J, Toscano KT, Wigg AM, Zhou S. Greenspan PD, et al. Among authors: tommasi ra. Bioorg Med Chem Lett. 2003 Nov 17;13(22):4121-4. doi: 10.1016/j.bmcl.2003.08.006. Bioorg Med Chem Lett. 2003. PMID: 14592520
Discovery of potent, selective, and orally active carboxylic acid based inhibitors of matrix metalloproteinase-13.
Monovich LG, Tommasi RA, Fujimoto RA, Blancuzzi V, Clark K, Cornell WD, Doti R, Doughty J, Fang J, Farley D, Fitt J, Ganu V, Goldberg R, Goldstein R, Lavoie S, Kulathila R, Macchia W, Parker DT, Melton R, O'Byrne E, Pastor G, Pellas T, Quadros E, Reel N, Roland DM, Sakane Y, Singh H, Skiles J, Somers J, Toscano K, Wigg A, Zhou S, Zhu L, Shieh WC, Xue S, McQuire LW. Monovich LG, et al. Among authors: tommasi ra. J Med Chem. 2009 Jun 11;52(11):3523-38. doi: 10.1021/jm801394m. J Med Chem. 2009. PMID: 19422229
Potent and selective 2-naphthylsulfonamide substituted hydroxamic acid inhibitors of matrix metalloproteinase-13.
Tommasi RA, Weiler S, McQuire LW, Rogel O, Chambers M, Clark K, Doughty J, Fang J, Ganu V, Grob J, Goldberg R, Goldstein R, Lavoie S, Kulathila R, Macchia W, Melton R, Springer C, Walker M, Zhang J, Zhu L, Shultz M. Tommasi RA, et al. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6440-5. doi: 10.1016/j.bmcl.2011.08.087. Epub 2011 Aug 27. Bioorg Med Chem Lett. 2011. PMID: 21937229
Optimization of halopemide for phospholipase D2 inhibition.
Monovich L, Mugrage B, Quadros E, Toscano K, Tommasi R, LaVoie S, Liu E, Du Z, LaSala D, Boyar W, Steed P. Monovich L, et al. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2310-1. doi: 10.1016/j.bmcl.2007.01.059. Epub 2007 Jan 25. Bioorg Med Chem Lett. 2007. PMID: 17317170
Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC.
Piizzi G, Parker DT, Peng Y, Dobler M, Patnaik A, Wattanasin S, Liu E, Lenoir F, Nunez J, Kerrigan J, McKenney D, Osborne C, Yu D, Lanieri L, Bojkovic J, Dzink-Fox J, Lilly MD, Sprague ER, Lu Y, Wang H, Ranjitkar S, Xie L, Wang B, Glick M, Hamann LG, Tommasi R, Yang X, Dean CR. Piizzi G, et al. J Med Chem. 2017 Jun 22;60(12):5002-5014. doi: 10.1021/acs.jmedchem.7b00377. Epub 2017 Jun 9. J Med Chem. 2017. PMID: 28549219
Structure-based design of HIV protease inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones as effective, nonpeptidic inhibitors.
Thaisrivongs S, Romero DL, Tommasi RA, Janakiraman MN, Strohbach JW, Turner SR, Biles C, Morge RR, Johnson PD, Aristoff PA, Tomich PK, Lynn JC, Horng MM, Chong KT, Hinshaw RR, Howe WJ, Finzel BC, Watenpaugh KD. Thaisrivongs S, et al. Among authors: tommasi ra. J Med Chem. 1996 Nov 8;39(23):4630-42. doi: 10.1021/jm960228q. J Med Chem. 1996. PMID: 8917652
Human HDAC isoform selectivity achieved via exploitation of the acetate release channel with structurally unique small molecule inhibitors.
Whitehead L, Dobler MR, Radetich B, Zhu Y, Atadja PW, Claiborne T, Grob JE, McRiner A, Pancost MR, Patnaik A, Shao W, Shultz M, Tichkule R, Tommasi RA, Vash B, Wang P, Stams T. Whitehead L, et al. Among authors: tommasi ra. Bioorg Med Chem. 2011 Aug 1;19(15):4626-34. doi: 10.1016/j.bmc.2011.06.030. Epub 2011 Jun 15. Bioorg Med Chem. 2011. PMID: 21723733
1-Alkyl-4-phenyl-6-alkoxy-1H-quinazolin-2-ones: a novel series of potent calcium-sensing receptor antagonists.
Widler L, Altmann E, Beerli R, Breitenstein W, Bouhelal R, Buhl T, Gamse R, Gerspacher M, Halleux C, John MR, Lehmann H, Kalb O, Kneissel M, Missbach M, Müller IR, Reidemeister S, Renaud J, Taillardat A, Tommasi R, Weiler S, Wolf RM, Seuwen K. Widler L, et al. J Med Chem. 2010 Mar 11;53(5):2250-63. doi: 10.1021/jm901811v. J Med Chem. 2010. PMID: 20158186
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Naik M, Humnabadkar V, Tantry SJ, Panda M, Narayan A, Guptha S, Panduga V, Manjrekar P, Jena LK, Koushik K, Shanbhag G, Jatheendranath S, Manjunatha MR, Gorai G, Bathula C, Rudrapatna S, Achar V, Sharma S, Ambady A, Hegde N, Mahadevaswamy J, Kaur P, Sambandamurthy VK, Awasthy D, Narayan C, Ravishankar S, Madhavapeddi P, Reddy J, Prabhakar K, Saralaya R, Chatterji M, Whiteaker J, McLaughlin B, Chiarelli LR, Riccardi G, Pasca MR, Binda C, Neres J, Dhar N, Signorino-Gelo F, McKinney JD, Ramachandran V, Shandil R, Tommasi R, Iyer PS, Narayanan S, Hosagrahara V, Kavanagh S, Dinesh N, Ghorpade SR. Naik M, et al. J Med Chem. 2014 Jun 26;57(12):5419-34. doi: 10.1021/jm5005978. Epub 2014 Jun 11. J Med Chem. 2014. PMID: 24871036
37 results