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Items: 1 to 20 of 97

1.

Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis.

Lou Y, Han X, Kuglstatter A, Kondru RK, Sweeney ZK, Soth M, McIntosh J, Litman R, Suh J, Kocer B, Davis D, Park J, Frauchiger S, Dewdney N, Zecic H, Taygerly JP, Sarma K, Hong J, Hill RJ, Gabriel T, Goldstein DM, Owens TD.

J Med Chem. 2015 Jan 8;58(1):512-6. doi: 10.1021/jm500305p.

PMID:
24712864
2.

Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton's tyrosine kinase inhibitors.

Zhao X, Xin M, Huang W, Ren Y, Jin Q, Tang F, Jiang H, Wang Y, Yang J, Mo S, Xiang H.

Bioorg Med Chem. 2015 Jan 15;23(2):348-64. doi: 10.1016/j.bmc.2014.11.006.

PMID:
25515957
3.

Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.

Kim KH, Maderna A, Schnute ME, Hegen M, Mohan S, Miyashiro J, Lin L, Li E, Keegan S, Lussier J, Wrocklage C, Nickerson-Nutter CL, Wittwer AJ, Soutter H, Caspers N, Han S, Kurumbail R, Dunussi-Joannopoulos K, Douhan J 3rd, Wissner A.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6258-63. doi: 10.1016/j.bmcl.2011.09.008.

PMID:
21958547
4.

Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.

Lou Y, Sweeney ZK, Kuglstatter A, Davis D, Goldstein DM, Han X, Hong J, Kocer B, Kondru RK, Litman R, McIntosh J, Sarma K, Suh J, Taygerly J, Owens TD.

Bioorg Med Chem Lett. 2015 Jan 15;25(2):367-71. doi: 10.1016/j.bmcl.2014.11.030.

PMID:
25466710
5.

RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents.

Xu D, Kim Y, Postelnek J, Vu MD, Hu DQ, Liao C, Bradshaw M, Hsu J, Zhang J, Pashine A, Srinivasan D, Woods J, Levin A, O'Mahony A, Owens TD, Lou Y, Hill RJ, Narula S, DeMartino J, Fine JS.

J Pharmacol Exp Ther. 2012 Apr;341(1):90-103. doi: 10.1124/jpet.111.187740.

6.

Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold.

Zhao X, Huang W, Wang Y, Xin M, Jin Q, Cai J, Tang F, Zhao Y, Xiang H.

Bioorg Med Chem. 2015 Feb 15;23(4):891-901. doi: 10.1016/j.bmc.2014.10.043.

PMID:
25596757
7.
8.
9.

Design and synthesis of carbazole carboxamides as promising inhibitors of Bruton's tyrosine kinase (BTK) and Janus kinase 2 (JAK2).

Liu Q, Batt DG, Lippy JS, Surti N, Tebben AJ, Muckelbauer JK, Chen L, An Y, Chang C, Pokross M, Yang Z, Wang H, Burke JR, Carter PH, Tino JA.

Bioorg Med Chem Lett. 2015 Oct 1;25(19):4265-9. doi: 10.1016/j.bmcl.2015.07.102.

PMID:
26320619
10.

Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.

Huang Z, Zhang Q, Yan L, Zhong G, Zhang L, Tan X, Wang Y.

Bioorg Med Chem Lett. 2016 Apr 15;26(8):1954-7. doi: 10.1016/j.bmcl.2016.03.011.

PMID:
26976214
11.

Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase.

Mina-Osorio P, LaStant J, Keirstead N, Whittard T, Ayala J, Stefanova S, Garrido R, Dimaano N, Hilton H, Giron M, Lau KY, Hang J, Postelnek J, Kim Y, Min S, Patel A, Woods J, Ramanujam M, DeMartino J, Narula S, Xu D.

Arthritis Rheum. 2013 Sep;65(9):2380-91. doi: 10.1002/art.38047.

12.

Bruton's tyrosine kinase as a drug discovery target.

Pan Z.

Drug News Perspect. 2008 Sep;21(7):357-62. doi: 10.1358/dnp.2008.21.7.1255308. Review.

PMID:
19259548
13.

Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase.

Pan Z, Scheerens H, Li SJ, Schultz BE, Sprengeler PA, Burrill LC, Mendonca RV, Sweeney MD, Scott KC, Grothaus PG, Jeffery DA, Spoerke JM, Honigberg LA, Young PR, Dalrymple SA, Palmer JT.

ChemMedChem. 2007 Jan;2(1):58-61. No abstract available.

PMID:
17154430
14.

Fragment-Based Discovery of a Small Molecule Inhibitor of Bruton's Tyrosine Kinase.

Smith CR, Dougan DR, Komandla M, Kanouni T, Knight B, Lawson JD, Sabat M, Taylor ER, Vu P, Wyrick C.

J Med Chem. 2015 Jul 23;58(14):5437-44. doi: 10.1021/acs.jmedchem.5b00734.

PMID:
26087137
15.

Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors.

Zhao X, Huang W, Wang Y, Xin M, Jin Q, Cai J, Tang F, Zhao Y, Xiang H.

Bioorg Med Chem. 2015 Aug 1;23(15):4344-53. doi: 10.1016/j.bmc.2015.06.023.

PMID:
26169764
16.

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.

Bioorg Med Chem Lett. 2014 May 1;24(9):2206-11. doi: 10.1016/j.bmcl.2014.02.075.

PMID:
24685542
17.

Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.

Young WB, Barbosa J, Blomgren P, Bremer MC, Crawford JJ, Dambach D, Gallion S, Hymowitz SG, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Maurer B, Mitchell SA, Ortwine DF, Di Paolo J, Reif K, Scheerens H, Schmitt A, Sowell CG, Wang X, Wong H, Xiong JM, Xu J, Zhao Z, Currie KS.

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1333-7. doi: 10.1016/j.bmcl.2015.01.032.

PMID:
25701252
18.

TR-FRET binding assay targeting unactivated form of Bruton's tyrosine kinase.

Asami T, Kawahata W, Sawa M.

Bioorg Med Chem Lett. 2015;25(10):2033-6. doi: 10.1016/j.bmcl.2015.04.001.

PMID:
25872980
19.

Investigational Bruton's tyrosine kinase inhibitors for the treatment of rheumatoid arthritis.

Norman P.

Expert Opin Investig Drugs. 2016 Aug;25(8):891-9. doi: 10.1080/13543784.2016.1182499. Review.

PMID:
27148767
20.

QSAR analysis of nicotinamidic compounds and design of potential Bruton's tyrosine kinase (Btk) inhibitors.

Santos-Garcia L, Assis LC, Silva DR, Ramalho TC, da Cunha EF.

J Biomol Struct Dyn. 2016 Jul;34(7):1421-40. doi: 10.1080/07391102.2015.1070750.

PMID:
26305710

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