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Page 1
The discovery of anthranilic acid-based MMP inhibitors. Part 2: SAR of the 5-position and P1(1) groups.
Levin JI, Chen J, Du M, Hogan M, Kincaid S, Nelson FC, Venkatesan AM, Wehr T, Zask A, DiJoseph J, Killar LM, Skala S, Sung A, Sharr M, Roth C, Jin G, Cowling R, Mohler KM, Black RA, March CJ, Skotnicki JS. Levin JI, et al. Among authors: skala s. Bioorg Med Chem Lett. 2001 Aug 20;11(16):2189-92. doi: 10.1016/s0960-894x(01)00419-x. Bioorg Med Chem Lett. 2001. PMID: 11514167
The discovery of anthranilic acid-based MMP inhibitors. Part 3: incorporation of basic amines.
Levin JI, Chen JM, Du MT, Nelson FC, Wehr T, DiJoseph JF, Killar LM, Skala S, Sung A, Sharr MA, Roth CE, Jin G, Cowling R, Di L, Sherman M, Xu ZB, March CJ, Mohler KM, Black RA, Skotnicki JS. Levin JI, et al. Among authors: skala s. Bioorg Med Chem Lett. 2001 Nov 19;11(22):2975-8. doi: 10.1016/s0960-894x(01)00601-1. Bioorg Med Chem Lett. 2001. PMID: 11677139
Synthesis and SAR of bicyclic heteroaryl hydroxamic acid MMP and TACE inhibitors.
Zask A, Gu Y, Albright JD, Du X, Hogan M, Levin JI, Chen JM, Killar LM, Sung A, DiJoseph JF, Sharr MA, Roth CE, Skala S, Jin G, Cowling R, Mohler KM, Barone D, Black R, March C, Skotnicki JS. Zask A, et al. Among authors: skala s. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1487-90. doi: 10.1016/s0960-894x(03)00127-6. Bioorg Med Chem Lett. 2003. PMID: 12668018
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.
Qin LY, Ruan Z, Cherney RJ, Dhar TGM, Neels J, Weigelt CA, Sack JS, Srivastava AS, Cornelius LAM, Tino JA, Stefanski K, Gu X, Xie J, Susulic V, Yang X, Yarde-Chinn M, Skala S, Bosnius R, Goldstein C, Davies P, Ruepp S, Salter-Cid L, Bhide RS, Poss MA. Qin LY, et al. Among authors: skala s. Bioorg Med Chem Lett. 2017 Feb 15;27(4):855-861. doi: 10.1016/j.bmcl.2017.01.016. Epub 2017 Jan 10. Bioorg Med Chem Lett. 2017. PMID: 28108251
Discovery and SAR of pyrrolo[2,1-f][1,2,4]triazin-4-amines as potent and selective PI3Kδ inhibitors.
Bhide RS, Neels J, Qin LY, Ruan Z, Stachura S, Weigelt C, Sack JS, Stefanski K, Gu X, Xie JH, Goldstine CB, Skala S, Pedicord DL, Ruepp S, Dhar TG, Carter PH, Salter-Cid LM, Poss MA, Davies P. Bhide RS, et al. Among authors: skala s. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4256-60. doi: 10.1016/j.bmcl.2016.07.047. Epub 2016 Jul 21. Bioorg Med Chem Lett. 2016. PMID: 27476421
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. Among authors: skala s. 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 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. Among authors: skala s. 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
De novo design, synthesis, and in vitro activity of LFA-1 antagonists based on a bicyclic[5.5]hydantoin scaffold.
Potin D, Launay M, Nicolai E, Fabreguette M, Malabre P, Caussade F, Besse D, Skala S, Stetsko DK, Todderud G, Beno BR, Cheney DL, Chang CJ, Sheriff S, Hollenbaugh DL, Barrish JC, Iwanowicz EJ, Suchard SJ, Dhar TG. Potin D, et al. Among authors: skala s. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1161-4. doi: 10.1016/j.bmcl.2004.12.007. Bioorg Med Chem Lett. 2005. PMID: 15686933
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: skala s. J Med Chem. 2010 May 13;53(9):3814-30. doi: 10.1021/jm100348u. J Med Chem. 2010. PMID: 20405922
81 results