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Quinic acid derivatives as sialyl Lewis(x)-mimicking selectin inhibitors: design, synthesis, and crystal structure in complex with E-selectin.
Kaila N, Somers WS, Thomas BE, Thakker P, Janz K, DeBernardo S, Tam S, Moore WJ, Yang R, Wrona W, Bedard PW, Crommie D, Keith JC Jr, Tsao DH, Alvarez JC, Ni H, Marchese E, Patton JT, Magnani JL, Camphausen RT. Kaila N, et al. J Med Chem. 2005 Jun 30;48(13):4346-57. doi: 10.1021/jm050049l. J Med Chem. 2005. PMID: 15974587
Beta-C-mannosides as selectin inhibitors.
Kaila N, Chen L, Thomas BE 4th, Tsao D, Tam S, Bedard PW, Camphausen RT, Alvarez JC, Ullas G. Kaila N, et al. J Med Chem. 2002 Apr 11;45(8):1563-6. doi: 10.1021/jm010390f. J Med Chem. 2002. PMID: 11931610
2-(4-Chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H]quinoline-4-carboxylic acid (PSI-697): identification of a clinical candidate from the quinoline salicylic acid series of P-selectin antagonists.
Kaila N, Janz K, Huang A, Moretto A, DeBernardo S, Bedard PW, Tam S, Clerin V, Keith JC Jr, Tsao DH, Sushkova N, Shaw GD, Camphausen RT, Schaub RG, Wang Q. Kaila N, et al. J Med Chem. 2007 Jan 11;50(1):40-64. doi: 10.1021/jm060631p. J Med Chem. 2007. PMID: 17201409
Discovery of 2-[1-(4-chlorophenyl)cyclopropyl]-3-hydroxy-8-(trifluoromethyl)quinoline-4-carboxylic acid (PSI-421), a P-selectin inhibitor with improved pharmacokinetic properties and oral efficacy in models of vascular injury.
Huang A, Moretto A, Janz K, Lowe M, Bedard PW, Tam S, Di L, Clerin V, Sushkova N, Tchernychev B, Tsao DH, Keith JC, Shaw GD, Schaub RG, Wang Q, Kaila N. Huang A, et al. Among authors: kaila n. J Med Chem. 2010 Aug 26;53(16):6003-17. doi: 10.1021/jm9013696. J Med Chem. 2010. PMID: 20718494
Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.
Gavrin LK, Green N, Hu Y, Janz K, Kaila N, Li HQ, Tam SY, Thomason JR, Gopalsamy A, Ciszewski G, Cuozzo JW, Hall JP, Hsu S, Telliez JB, Lin LL. Gavrin LK, et al. Among authors: kaila n. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5288-92. doi: 10.1016/j.bmcl.2005.08.029. Epub 2005 Sep 13. Bioorg Med Chem Lett. 2005. PMID: 16165349
41 results