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Page 1
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: delucca g. 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
Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA. Watterson SH, et al. J Med Chem. 2016 Oct 13;59(19):9173-9200. doi: 10.1021/acs.jmedchem.6b01088. Epub 2016 Sep 19. J Med Chem. 2016. PMID: 27583770
Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties.
Hill MD, Fang H, Norris D, Delucca GV, Huang H, DeBenedetto M, Quesnelle C, Schmitz WD, Tokarski JS, Sheriff S, Yan C, Fanslau C, Haarhoff Z, Huang C, Kramer M, Madari S, Menard K, Monereau L, Morrison J, Raghavan N, Shields EE, Simmermacher-Mayer J, Sinz M, Tye CK, Westhouse R, Xie C, Zhang H, Zhang L, Zvyaga T, Lee F, Gavai AV, Degnan AP. Hill MD, et al. Among authors: delucca gv. ACS Med Chem Lett. 2022 Jul 5;13(7):1165-1171. doi: 10.1021/acsmedchemlett.2c00219. eCollection 2022 Jul 14. ACS Med Chem Lett. 2022. PMID: 35859878 Free PMC article.
Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).
De Lucca GV, Shi Q, Liu Q, Batt DG, Beaudoin Bertrand M, Rampulla R, Mathur A, Discenza L, D'Arienzo C, Dai J, Obermeier M, Vickery R, Zhang Y, Yang Z, Marathe P, Tebben AJ, Muckelbauer JK, Chang CJ, Zhang H, Gillooly K, Taylor T, Pattoli MA, Skala S, Kukral DW, McIntyre KW, Salter-Cid L, Fura A, Burke JR, Barrish JC, Carter PH, Tino JA. De Lucca GV, et al. J Med Chem. 2016 Sep 8;59(17):7915-35. doi: 10.1021/acs.jmedchem.6b00722. Epub 2016 Aug 26. J Med Chem. 2016. PMID: 27531604
Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency.
De Lucca GV, Kim UT, Vargo BJ, Duncia JV, Santella JB 3rd, Gardner DS, Zheng C, Liauw A, Wang Z, Emmett G, Wacker DA, Welch PK, Covington M, Stowell NC, Wadman EA, Das AM, Davies P, Yeleswaram S, Graden DM, Solomon KA, Newton RC, Trainor GL, Decicco CP, Ko SS. De Lucca GV, et al. J Med Chem. 2005 Mar 24;48(6):2194-211. doi: 10.1021/jm049530m. J Med Chem. 2005. PMID: 15771462
Purine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors for autoimmune diseases.
Shi Q, Tebben A, Dyckman AJ, Li H, Liu C, Lin J, Spergel S, Burke JR, McIntyre KW, Olini GC, Strnad J, Surti N, Muckelbauer JK, Chang C, An Y, Cheng L, Ruan Q, Leftheris K, Carter PH, Tino J, De Lucca GV. Shi Q, et al. Bioorg Med Chem Lett. 2014 May 1;24(9):2206-11. doi: 10.1016/j.bmcl.2014.02.075. Epub 2014 Mar 13. Bioorg Med Chem Lett. 2014. PMID: 24685542
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.
Santella JB 3rd, Gardner DS, Yao W, Shi C, Reddy P, Tebben AJ, DeLucca GV, Wacker DA, Watson PS, Welch PK, Wadman EA, Davies P, Solomon KA, Graden DM, Yeleswaram S, Mandlekar S, Kariv I, Decicco CP, Ko SS, Carter PH, Duncia JV. Santella JB 3rd, et al. Among authors: delucca gv. Bioorg Med Chem Lett. 2008 Jan 15;18(2):576-85. doi: 10.1016/j.bmcl.2007.11.067. Epub 2007 Nov 22. Bioorg Med Chem Lett. 2008. PMID: 18096386
CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships.
Wacker DA, Santella JB 3rd, Gardner DS, Varnes JG, Estrella M, DeLucca GV, Ko SS, Tanabe K, Watson PS, Welch PK, Covington M, Stowell NC, Wadman EA, Davies P, Solomon KA, Newton RC, Trainor GL, Friedman SM, Decicco CP, Duncia JV. Wacker DA, et al. Among authors: delucca gv. Bioorg Med Chem Lett. 2002 Jul 8;12(13):1785-9. doi: 10.1016/s0960-894x(02)00206-8. Bioorg Med Chem Lett. 2002. PMID: 12067561
22 results