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Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design.
Gavai AV, Norris D, Delucca G, Tortolani D, Tokarski JS, Dodd D, O'Malley D, Zhao Y, Quesnelle C, Gill P, Vaccaro W, Huynh T, Ahuja V, Han WC, Mussari C, Harikrishnan L, Kamau M, Poss M, Sheriff S, Yan C, Marsilio F, Menard K, Wen ML, Rampulla R, Wu DR, Li J, Zhang H, Li P, Sun D, Yip H, Traeger SC, Zhang Y, Mathur A, Zhang H, Huang C, Yang Z, Ranasinghe A, Everlof G, Raghavan N, Tye CK, Wee S, Hunt JT, Vite G, Westhouse R, Lee FY. Gavai AV, et al. Among authors: tortolani d. J Med Chem. 2021 Oct 14;64(19):14247-14265. doi: 10.1021/acs.jmedchem.1c00625. Epub 2021 Sep 20. J Med Chem. 2021. PMID: 34543572
Pyrrolopyridazine MEK inhibitors.
Chen Z, Kim SH, Barbosa SA, Huynh T, Tortolani DR, Leavitt KJ, Wei DD, Manne V, Ricca CS, Gullo-Brown J, Poss MA, Vaccaro W, Salvati ME. Chen Z, et al. Among authors: tortolani dr. Bioorg Med Chem Lett. 2006 Feb;16(3):628-32. doi: 10.1016/j.bmcl.2005.10.052. Epub 2005 Nov 3. Bioorg Med Chem Lett. 2006. PMID: 16275076
Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl)nicotinic acid (BMS-688521).
Watterson SH, Xiao Z, Dodd DS, Tortolani DR, Vaccaro W, Potin D, Launay M, Stetsko DK, Skala S, Davis PM, Lee D, Yang X, McIntyre KW, Balimane P, Patel K, Yang Z, Marathe P, Kadiyala P, Tebben AJ, Sheriff S, Chang CY, Ziemba T, Zhang H, Chen BC, DelMonte AJ, Aranibar N, McKinnon M, Barrish JC, Suchard SJ, Murali Dhar TG. Watterson SH, et al. Among authors: tortolani dr. J Med Chem. 2010 May 13;53(9):3814-30. doi: 10.1021/jm100348u. J Med Chem. 2010. PMID: 20405922
Modulation of cofilin phosphorylation by inhibition of the Lim family kinases.
He L, Seitz SP, Trainor GL, Tortolani D, Vaccaro W, Poss M, Tarby CM, Tokarski JS, Penhallow B, Hung CY, Attar R, Lin TA. He L, et al. Among authors: tortolani d. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5995-8. doi: 10.1016/j.bmcl.2012.07.002. Epub 2012 Jul 21. Bioorg Med Chem Lett. 2012. PMID: 22902653
Multiple and single binding modes of fragment-like kinase inhibitors revealed by molecular modeling, residue type-selective protonation, and nuclear overhauser effects.
Constantine KL, Mueller L, Metzler WJ, McDonnell PA, Todderud G, Goldfarb V, Fan Y, Newitt JA, Kiefer SE, Gao M, Tortolani D, Vaccaro W, Tokarski J. Constantine KL, et al. Among authors: tortolani d. J Med Chem. 2008 Oct 9;51(19):6225-9. doi: 10.1021/jm800747w. Epub 2008 Sep 5. J Med Chem. 2008. PMID: 18771253
Long-Acting Tumor-Activated Prodrug of a TGFβR Inhibitor.
Zhang Y, Parrish KE, Tortolani DR, Poss MA, Huang A, Wan H, Purandare AV, Donnell AF, Kempson J, Hou X, Pawluczyk J, Yip S, Luk E, Raghavan N, Swanson J, Smalley J, Murtaza A, Yang Z, Augustine-Rauch K, Lombardo LJ, Borzilleri R. Zhang Y, et al. Among authors: tortolani dr. J Med Chem. 2021 Nov 11;64(21):15787-15798. doi: 10.1021/acs.jmedchem.0c02043. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704759
Aminotriazine 5-HT7 antagonists.
Mattson RJ, Denhart DJ, Catt JD, Dee MF, Deskus JA, Ditta JL, Epperson J, Dalton King H, Gao A, Poss MA, Purandare A, Tortolani D, Zhao Y, Yang H, Yeola S, Palmer J, Torrente J, Stark A, Johnson G. Mattson RJ, et al. Among authors: tortolani d. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4245-8. doi: 10.1016/j.bmcl.2004.06.008. Bioorg Med Chem Lett. 2004. PMID: 15261279
36 results