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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. Among authors: tsao dh. 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: tsao dh. 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: tsao dh. J Med Chem. 2010 Aug 26;53(16):6003-17. doi: 10.1021/jm9013696. J Med Chem. 2010. PMID: 20718494
Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors.
Cole DC, Asselin M, Brennan A, Czerwinski R, Ellingboe JW, Fitz L, Greco R, Huang X, Joseph-McCarthy D, Kelly MF, Kirisits M, Lee J, Li Y, Morgan P, Stock JR, Tsao DH, Wissner A, Yang X, Chaudhary D. Cole DC, et al. Among authors: tsao dh. J Med Chem. 2008 Oct 9;51(19):5958-63. doi: 10.1021/jm800214a. Epub 2008 Sep 11. J Med Chem. 2008. PMID: 18783200
Combinatorial synthesis of substituted 3-(2-indolyl)piperidines and 2-phenyl indoles as inhibitors of ZipA-FtsZ interaction.
Jennings LD, Foreman KW, Rush TS 3rd, Tsao DH, Mosyak L, Kincaid SL, Sukhdeo MN, Sutherland AG, Ding W, Kenny CH, Sabus CL, Liu H, Dushin EG, Moghazeh SL, Labthavikul P, Petersen PJ, Tuckman M, Haney SA, Ruzin AV. Jennings LD, et al. Among authors: tsao dh. Bioorg Med Chem. 2004 Oct 1;12(19):5115-31. doi: 10.1016/j.bmc.2004.07.031. Bioorg Med Chem. 2004. PMID: 15351395
38 results