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Items: 1 to 20 of 90

1.

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
2.

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
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.

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
5.

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
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.

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
9.

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
10.

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
11.

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
12.

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
13.

Structure-based design and synthesis of potent benzothiazole inhibitors of interleukin-2 inducible T cell kinase (ITK).

MacKinnon CH, Lau K, Burch JD, Chen Y, Dines J, Ding X, Eigenbrot C, Heifetz A, Jaochico A, Johnson A, Kraemer J, Kruger S, Krülle TM, Liimatta M, Ly J, Maghames R, Montalbetti CA, Ortwine DF, Pérez-Fuertes Y, Shia S, Stein DB, Trani G, Vaidya DG, Wang X, Bromidge SM, Wu LC, Pei Z.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6331-5. doi: 10.1016/j.bmcl.2013.09.069. Epub 2013 Oct 1.

PMID:
24138940
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
17.

Inhibition of the IL-2-inducible tyrosine kinase (Itk) activity: a new concept for the therapy of inflammatory skin diseases.

von Bonin A, Rausch A, Mengel A, Hitchcock M, Krüger M, von Ahsen O, Merz C, Röse L, Stock C, Martin SF, Leder G, Döcke WD, Asadullah K, Zügel U.

Exp Dermatol. 2011 Jan;20(1):41-7. doi: 10.1111/j.1600-0625.2010.01198.x.

PMID:
21158938
18.

Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties.

Charles MD, Brookfield JL, Ekwuru TC, Stockley M, Dunn J, Riddick M, Hammonds T, Trivier E, Greenland G, Wong AC, Cheasty A, Boyd S, Crighton D, Olson MF.

J Med Chem. 2015 Oct 22;58(20):8309-13. doi: 10.1021/acs.jmedchem.5b01242. Epub 2015 Sep 30.

PMID:
26356364
19.

5-Aminomethylbenzimidazoles as potent ITK antagonists.

Riether D, Zindell R, Kowalski JA, Cook BN, Bentzien J, Lombaert SD, Thomson D, Kugler SZ Jr, Skow D, Martin LS, Raymond EL, Khine HH, O'Shea K, Woska JR Jr, Jeanfavre D, Sellati R, Ralph KL, Ahlberg J, Labissiere G, Kashem MA, Pullen SS, Takahashi H.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1588-91. doi: 10.1016/j.bmcl.2009.02.012. Epub 2009 Feb 8.

PMID:
19246196
20.

Covalent modification of cyclooxygenase-2 (COX-2) by 2-acetoxyphenyl alkyl sulfides, a new class of selective COX-2 inactivators.

Kalgutkar AS, Kozak KR, Crews BC, Hochgesang GP Jr, Marnett LJ.

J Med Chem. 1998 Nov 19;41(24):4800-18.

PMID:
9822550

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