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Page 1
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. Among authors: janz k. J Med Chem. 2005 Jun 30;48(13):4346-57. doi: 10.1021/jm050049l. J Med Chem. 2005. PMID: 15974587
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. Among authors: janz k. 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: janz k. 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: janz k. 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
Inhibitors of tumor progression loci-2 (Tpl2) kinase and tumor necrosis factor alpha (TNF-alpha) production: selectivity and in vivo antiinflammatory activity of novel 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles.
Green N, Hu Y, Janz K, Li HQ, Kaila N, Guler S, Thomason J, Joseph-McCarthy D, Tam SY, Hotchandani R, Wu J, Huang A, Wang Q, Leung L, Pelker J, Marusic S, Hsu S, Telliez JB, Hall JP, Cuozzo JW, Lin LL. Green N, et al. Among authors: janz k. J Med Chem. 2007 Sep 20;50(19):4728-45. doi: 10.1021/jm070436q. Epub 2007 Aug 23. J Med Chem. 2007. PMID: 17715908
Characterization of the novel P-selectin inhibitor PSI-697 [2-(4-chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[h] quinoline-4-carboxylic acid] in vitro and in rodent models of vascular inflammation and thrombosis.
Bedard PW, Clerin V, Sushkova N, Tchernychev B, Antrilli T, Resmini C, Keith JC Jr, Hennan JK, Kaila N, Debernardo S, Janz K, Wang Q, Crandall DL, Schaub RG, Shaw GD, Carter LL. Bedard PW, et al. Among authors: janz k. J Pharmacol Exp Ther. 2008 Feb;324(2):497-506. doi: 10.1124/jpet.107.128124. Epub 2007 Nov 16. J Pharmacol Exp Ther. 2008. PMID: 18024786
170 results