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Page 1
Structure-activity relationship (SAR) of the α-amino acid residue of potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonists.
Zhong M, Hanan EJ, Shen W, Bui M, Arkin MR, Barr KJ, Evanchik MJ, Hoch U, Hyde J, Martell JR, Oslob JD, Paulvannan K, Prabhu S, Silverman JA, Wright J, Yu CH, Zhu J, Flanagan WM. Zhong M, et al. Among authors: barr kj. Bioorg Med Chem Lett. 2011 Jan 1;21(1):307-10. doi: 10.1016/j.bmcl.2010.11.014. Epub 2010 Nov 5. Bioorg Med Chem Lett. 2011. PMID: 21109434
Design and synthesis of 2-amino-pyrazolopyridines as Polo-like kinase 1 inhibitors.
Fucini RV, Hanan EJ, Romanowski MJ, Elling RA, Lew W, Barr KJ, Zhu J, Yoburn JC, Liu Y, Fahr BT, Fan J, Lu Y, Pham P, Choong IC, VanderPorten EC, Bui M, Purkey HE, Evanchik MJ, Yang W. Fucini RV, et al. Among authors: barr kj. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5648-52. doi: 10.1016/j.bmcl.2008.08.095. Epub 2008 Aug 29. Bioorg Med Chem Lett. 2008. PMID: 18793847
Discovery of tetrahydroisoquinoline (THIQ) derivatives as potent and orally bioavailable LFA-1/ICAM-1 antagonists.
Zhong M, Shen W, Barr KJ, Arbitrario JP, Arkin MR, Bui M, Chen T, Cunningham BC, Evanchik MJ, Hanan EJ, Hoch U, Huen K, Hyde J, Kumer JL, Lac T, Lawrence CE, Martell JR, Oslob JD, Paulvannan K, Prabhu S, Silverman JA, Wright J, Yu CH, Zhu J, Flanagan WM. Zhong M, et al. Among authors: barr kj. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5269-73. doi: 10.1016/j.bmcl.2010.06.145. Epub 2010 Jul 23. Bioorg Med Chem Lett. 2010. PMID: 20655213
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
Zhong M, Gadek TR, Bui M, Shen W, Burnier J, Barr KJ, Hanan EJ, Oslob JD, Yu CH, Zhu J, Arkin MR, Evanchik MJ, Flanagan WM, Hoch U, Hyde J, Prabhu S, Silverman JA, Wright J. Zhong M, et al. Among authors: barr kj. ACS Med Chem Lett. 2012 Jan 31;3(3):203-6. doi: 10.1021/ml2002482. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900456 Free PMC article.
Structure of the Brachydanio rerio Polo-like kinase 1 (Plk1) catalytic domain in complex with an extended inhibitor targeting the adaptive pocket of the enzyme.
Elling RA, Fucini RV, Hanan EJ, Barr KJ, Zhu J, Paulvannan K, Yang W, Romanowski MJ. Elling RA, et al. Among authors: barr kj. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2008 Aug 1;64(Pt 8):686-91. doi: 10.1107/S1744309108019623. Epub 2008 Jul 26. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2008. PMID: 18678933 Free PMC article.
Allosteric inhibition of protein tyrosine phosphatase 1B.
Wiesmann C, Barr KJ, Kung J, Zhu J, Erlanson DA, Shen W, Fahr BJ, Zhong M, Taylor L, Randal M, McDowell RS, Hansen SK. Wiesmann C, et al. Among authors: barr kj. Nat Struct Mol Biol. 2004 Aug;11(8):730-7. doi: 10.1038/nsmb803. Epub 2004 Jul 18. Nat Struct Mol Biol. 2004. PMID: 15258570
Potent, orally active heterocycle-based combretastatin A-4 analogues: synthesis, structure-activity relationship, pharmacokinetics, and in vivo antitumor activity evaluation.
Wang L, Woods KW, Li Q, Barr KJ, McCroskey RW, Hannick SM, Gherke L, Credo RB, Hui YH, Marsh K, Warner R, Lee JY, Zielinski-Mozng N, Frost D, Rosenberg SH, Sham HL. Wang L, et al. Among authors: barr kj. J Med Chem. 2002 Apr 11;45(8):1697-711. doi: 10.1021/jm010523x. J Med Chem. 2002. PMID: 11931625
Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor.
Caravella JA, Lin J, Diebold RB, Campbell AM, Ericsson A, Gustafson G, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Kershaw M, Yao L, Toms AV, Barr KJ, Dinsmore CJ, Walker D, Ashwell S, Lu W. Caravella JA, et al. Among authors: barr kj. J Med Chem. 2020 Feb 27;63(4):1612-1623. doi: 10.1021/acs.jmedchem.9b01423. Epub 2020 Feb 12. J Med Chem. 2020. PMID: 31971798
Synthesis and biological evaluation of 2-indolyloxazolines as a new class of tubulin polymerization inhibitors. Discovery of A-289099 as an orally active antitumor agent.
Li Q, Woods KW, Claiborne A, Gwaltney SL 2nd, Barr KJ, Liu G, Gehrke L, Credo RB, Hui YH, Lee J, Warner RB, Kovar P, Nukkala MA, Zielinski NA, Tahir SK, Fitzgerald M, Kim KH, Marsh K, Frost D, Ng SC, Rosenberg S, Sham HL. Li Q, et al. Among authors: barr kj. Bioorg Med Chem Lett. 2002 Feb 11;12(3):465-9. doi: 10.1016/s0960-894x(01)00759-4. Bioorg Med Chem Lett. 2002. PMID: 11814821
Discovery and Optimization of Quinolinone Derivatives as Potent, Selective, and Orally Bioavailable Mutant Isocitrate Dehydrogenase 1 (mIDH1) Inhibitors.
Lin J, Lu W, Caravella JA, Campbell AM, Diebold RB, Ericsson A, Fritzen E, Gustafson GR, Lancia DR Jr, Shelekhin T, Wang Z, Castro J, Clarke A, Gotur D, Josephine HR, Katz M, Diep H, Kershaw M, Yao L, Kauffman G, Hubbs SE, Luke GP, Toms AV, Wang L, Bair KW, Barr KJ, Dinsmore C, Walker D, Ashwell S. Lin J, et al. Among authors: barr kj. J Med Chem. 2019 Jul 25;62(14):6575-6596. doi: 10.1021/acs.jmedchem.9b00362. Epub 2019 Jul 8. J Med Chem. 2019. PMID: 31199148
52 results