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Items: 1 to 20 of 130

1.

Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.

Das J, Liu C, Moquin RV, Lin J, Furch JA, Spergel SH, Doweyko AM, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Kanner SB, Lin TA, Dodd JH, Barrish JC, Wityak J.

Bioorg Med Chem Lett. 2006 May 1;16(9):2411-5. Epub 2006 Feb 14. Erratum in: Bioorg Med Chem Lett. 2006 Aug 1;16(15):4148. Doweyko, Arthur M [added].

PMID:
16481166
2.

Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors.

Das J, Furch JA, Liu C, Moquin RV, Lin J, Spergel SH, McIntyre KW, Shuster DJ, O'Day KD, Penhallow B, Hung CY, Doweyko AM, Kamath A, Zhang H, Marathe P, Kanner SB, Lin TA, Dodd JH, Barrish JC, Wityak J.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3706-12. Epub 2006 May 6.

PMID:
16682193
3.

Selective Itk inhibitors block T-cell activation and murine lung inflammation.

Lin TA, McIntyre KW, Das J, Liu C, O'Day KD, Penhallow B, Hung CY, Whitney GS, Shuster DJ, Yang X, Townsend R, Postelnek J, Spergel SH, Lin J, Moquin RV, Furch JA, Kamath AV, Zhang H, Marathe PH, Perez-Villar JJ, Doweyko A, Killar L, Dodd JH, Barrish JC, Wityak J, Kanner SB.

Biochemistry. 2004 Aug 31;43(34):11056-62.

PMID:
15323564
4.

Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.

Das J, Lin J, Moquin RV, Shen Z, Spergel SH, Wityak J, Doweyko AM, DeFex HF, Fang Q, Pang S, Pitt S, Shen DR, Schieven GL, Barrish JC.

Bioorg Med Chem Lett. 2003 Jul 7;13(13):2145-9.

PMID:
12798323
5.

Discovery of 2-amino-heteroaryl-benzothiazole-6-anilides as potent p56(lck) inhibitors.

Das J, Moquin RV, Lin J, Liu C, Doweyko AM, DeFex HF, Fang Q, Pang S, Pitt S, Shen DR, Schieven GL, Barrish JC, Wityak J.

Bioorg Med Chem Lett. 2003 Aug 4;13(15):2587-90.

PMID:
12852972
6.

Discovery, SAR and X-ray structure of 1H-benzimidazole-5-carboxylic acid cyclohexyl-methyl-amides as inhibitors of inducible T-cell kinase (Itk).

Moriarty KJ, Takahashi H, Pullen SS, Khine HH, Sallati RH, Raymond EL, Woska JR Jr, Jeanfavre DD, Roth GP, Winters MP, Qiao L, Ryan D, DesJarlais R, Robinson D, Wilson M, Bobko M, Cook BN, Lo HY, Nemoto PA, Kashem MA, Wolak JP, White A, Magolda RL, Tomczuk B.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5545-9. doi: 10.1016/j.bmcl.2008.09.015. Epub 2008 Sep 7. Erratum in: Bioorg Med Chem Lett. 2009 Mar 15;19(6):1835.

PMID:
18819799
7.

Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

Wityak J, Das J, Moquin RV, Shen Z, Lin J, Chen P, Doweyko AM, Pitt S, Pang S, Shen DR, Fang Q, de Fex HF, Schieven GL, Kanner SB, Barrish JC.

Bioorg Med Chem Lett. 2003 Nov 17;13(22):4007-10.

PMID:
14592495
8.

Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.

Cook BN, Bentzien J, White A, Nemoto PA, Wang J, Man CC, Soleymanzadeh F, Khine HH, Kashem MA, Kugler SZ Jr, Wolak JP, Roth GP, De Lombaert S, Pullen SS, Takahashi H.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):773-7. doi: 10.1016/j.bmcl.2008.12.028. Epub 2008 Dec 10.

PMID:
19111460
9.

Synthesis and structure-activity relationships of a series of novel thiazoles as inhibitors of aminoacyl-tRNA synthetases.

Yu XY, Hill JM, Yu G, Wang W, Kluge AF, Wendler P, Gallant P.

Bioorg Med Chem Lett. 1999 Feb 8;9(3):375-80.

PMID:
10091687
10.

5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk).

Winters MP, Robinson DJ, Khine HH, Pullen SS, Woska JR Jr, Raymond EL, Sellati R, Cywin CL, Snow RJ, Kashem MA, Wolak JP, King J, Kaplita PV, Liu LH, Farrell TM, DesJarlais R, Roth GP, Takahashi H, Moriarty KJ.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5541-4. doi: 10.1016/j.bmcl.2008.09.016. Epub 2008 Sep 7.

PMID:
18823779
11.

Inhibition of p56(lck) tyrosine kinase by isothiazolones.

Trevillyan JM, Chiou XG, Ballaron SJ, Tang QM, Buko A, Sheets MP, Smith ML, Putman CB, Wiedeman P, Tu N, Madar D, Smith HT, Gubbins EJ, Warrior UP, Chen YW, Mollison KW, Faltynek CR, Djurić SW.

Arch Biochem Biophys. 1999 Apr 1;364(1):19-29.

PMID:
10087161
12.

Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).

Farmer LJ, Bemis G, Britt SD, Cochran J, Connors M, Harrington EM, Hoock T, Markland W, Nanthakumar S, Taslimi P, Ter Haar E, Wang J, Zhaveri D, Salituro FG.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6231-5. doi: 10.1016/j.bmcl.2008.09.106. Epub 2008 Oct 7.

PMID:
18938080
13.

Discovery and structure-activity relationship of 3-aminopyrid-2-ones as potent and selective interleukin-2 inducible T-cell kinase (Itk) inhibitors.

Charrier JD, Miller A, Kay DP, Brenchley G, Twin HC, Collier PN, Ramaya S, Keily SB, Durrant SJ, Knegtel RM, Tanner AJ, Brown K, Curnock AP, Jimenez JM.

J Med Chem. 2011 Apr 14;54(7):2341-50. doi: 10.1021/jm101499u. Epub 2011 Mar 10.

PMID:
21391610
14.

Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors.

Pastor RM, Burch JD, Magnuson S, Ortwine DF, Chen Y, De La Torre K, Ding X, Eigenbrot C, Johnson A, Liimatta M, Liu Y, Shia S, Wang X, Wu LC, Pei Z.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2448-52. doi: 10.1016/j.bmcl.2014.04.023. Epub 2014 Apr 16.

PMID:
24767842
15.

Structure-activity relationship study of a novel necroptosis inhibitor, necrostatin-7.

Zheng W, Degterev A, Hsu E, Yuan J, Yuan C.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4932-5. doi: 10.1016/j.bmcl.2008.08.058. Epub 2008 Aug 22.

PMID:
18768316
16.

Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part I: Discovery of 3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide.

Uto Y, Ogata T, Harada J, Kiyotsuka Y, Ueno Y, Miyazawa Y, Kurata H, Deguchi T, Watanabe N, Takagi T, Wakimoto S, Okuyama R, Abe M, Kurikawa N, Kawamura S, Yamato M, Osumi J.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4151-8. doi: 10.1016/j.bmcl.2009.05.119. Epub 2009 Jun 2.

PMID:
19540759
17.

Identification of potent ITK inhibitors through focused compound library design including structural information.

Herdemann M, Heit I, Bosch FU, Quintini G, Scheipers C, Weber A.

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6998-7003. doi: 10.1016/j.bmcl.2010.09.119. Epub 2010 Sep 29.

PMID:
20965724
18.

Itk, a T cell-specific tyrosine kinase, is required for CD2-mediated interleukin-2 promoter activation in the human T cell line Jurkat.

Tanaka N, Abe H, Yagita H, Okumura K, Nakamura M, Sugamura K.

Eur J Immunol. 1997 Apr;27(4):834-41.

PMID:
9130632
19.

Synthesis of potent and selective inhibitors of Candida albicans N-myristoyltransferase based on the benzothiazole structure.

Yamazaki K, Kaneko Y, Suwa K, Ebara S, Nakazawa K, Yasuno K.

Bioorg Med Chem. 2005 Apr 1;13(7):2509-22.

PMID:
15755653
20.

Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.

Chen P, Norris D, Das J, Spergel SH, Wityak J, Leith L, Zhao R, Chen BC, Pitt S, Pang S, Shen DR, Zhang R, De Fex HF, Doweyko AM, McIntyre KW, Shuster DJ, Behnia K, Schieven GL, Barrish JC.

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6061-6.

PMID:
15546730
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