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Items: 11

1.

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.

J Med Chem. 2010 Aug 26;53(16):6003-17. doi: 10.1021/jm9013696.

PMID:
20718494
2.

Selectin inhibitors: a patent review.

Bedard PW, Kaila N.

Expert Opin Ther Pat. 2010 Jun;20(6):781-93. doi: 10.1517/13543771003767468. Review.

PMID:
20408735
3.

Prophylactic P-selectin inhibition with PSI-421 promotes resolution of venous thrombosis without anticoagulation.

Meier TR, Myers DD Jr, Wrobleski SK, Zajkowski PJ, Hawley AE, Bedard PW, Ballard NE, Londy FJ, Kaila N, Vlasuk GP, Schaub RG, Wakefield TW.

Thromb Haemost. 2008 Feb;99(2):343-51. doi: 10.1160/TH07-10-0608.

PMID:
18278184
4.

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.

J Pharmacol Exp Ther. 2008 Feb;324(2):497-506. Epub 2007 Nov 16.

PMID:
18024786
5.

Resolution of venous thrombosis using a novel oral small-molecule inhibitor of P-selectin (PSI-697) without anticoagulation.

Myers DD Jr, Wrobleski SK, Longo C, Bedard PW, Kaila N, Shaw GD, Londy FJ, Rohrer SE, Fex BA, Zajkowski PJ, Meier TR, Hawley AE, Farris DM, Ballard NE, Henke PK, Schaub RG, Wakefield TW.

Thromb Haemost. 2007 Mar;97(3):400-7.

PMID:
17334507
6.

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.

J Med Chem. 2007 Jan 11;50(1):40-64.

PMID:
17201409
7.

Synthesis and biological evaluation of quinoline salicylic acids as P-selectin antagonists.

Kaila N, Janz K, DeBernardo S, Bedard PW, Camphausen RT, Tam S, Tsao DH, Keith JC Jr, Nickerson-Nutter C, Shilling A, Young-Sciame R, Wang Q.

J Med Chem. 2007 Jan 11;50(1):21-39.

PMID:
17201408
8.

Treatment with an oral small molecule inhibitor of P selectin (PSI-697) decreases vein wall injury in a rat stenosis model of venous thrombosis.

Myers DD Jr, Henke PK, Bedard PW, Wrobleski SK, Kaila N, Shaw G, Meier TR, Hawley AE, Schaub RG, Wakefield TW.

J Vasc Surg. 2006 Sep;44(3):625-32.

9.

Decreased venous thrombosis with an oral inhibitor of P selectin.

Myers DD Jr, Rectenwald JE, Bedard PW, Kaila N, Shaw GD, Schaub RG, Farris DM, Hawley AE, Wrobleski SK, Henke PK, Wakefield TW.

J Vasc Surg. 2005 Aug;42(2):329-36.

10.

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.

J Med Chem. 2005 Jun 30;48(13):4346-57.

PMID:
15974587
11.

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.

J Med Chem. 2002 Apr 11;45(8):1563-6.

PMID:
11931610

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