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Page 1
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. Moriarty KJ, et al. Among authors: roth gp. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5545-9. doi: 10.1016/j.bmcl.2008.09.015. Epub 2008 Sep 7. Bioorg Med Chem Lett. 2008. PMID: 18819799
Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.
Moriarty KJ, Winters M, Qiao L, Ryan D, DesJarlis R, Robinson D, Cook BN, Kashem MA, Kaplita PV, Liu LH, Farrell TM, Khine HH, King J, Pullen SS, Roth GP, Magolda R, Takahashi H. Moriarty KJ, et al. Among authors: roth gp. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5537-40. doi: 10.1016/j.bmcl.2008.09.017. Epub 2008 Sep 7. Bioorg Med Chem Lett. 2008. PMID: 18819794
Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor.
Maloney PR, Khan P, Hedrick M, Gosalia P, Milewski M, Li L, Roth GP, Sergienko E, Suyama E, Sugarman E, Nguyen K, Mehta A, Vasile S, Su Y, Stonich D, Nguyen H, Zeng FY, Novo AM, Vicchiarelli M, Diwan J, Chung TD, Smith LH, Pinkerton AB. Maloney PR, et al. Among authors: roth gp. Bioorg Med Chem Lett. 2012 Nov 1;22(21):6656-60. doi: 10.1016/j.bmcl.2012.08.105. Epub 2012 Sep 7. Bioorg Med Chem Lett. 2012. PMID: 23010269 Free PMC article.
Imidazole-derived agonists for the neurotensin 1 receptor.
Hershberger PM, Hedrick MP, Peddibhotla S, Mangravita-Novo A, Gosalia P, Li Y, Gray W, Vicchiarelli M, Smith LH, Chung TD, Thomas JB, Caron MG, Pinkerton AB, Barak LS, Roth GP. Hershberger PM, et al. Among authors: roth gp. Bioorg Med Chem Lett. 2014 Jan 1;24(1):262-7. doi: 10.1016/j.bmcl.2013.11.026. Epub 2013 Nov 21. Bioorg Med Chem Lett. 2014. PMID: 24332089 Free PMC article.
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. Winters MP, et al. Among authors: roth gp. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5541-4. doi: 10.1016/j.bmcl.2008.09.016. Epub 2008 Sep 7. Bioorg Med Chem Lett. 2008. PMID: 18823779
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. Cook BN, et al. Among authors: roth gp. Bioorg Med Chem Lett. 2009 Feb 1;19(3):773-7. doi: 10.1016/j.bmcl.2008.12.028. Epub 2008 Dec 10. Bioorg Med Chem Lett. 2009. PMID: 19111460
Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules.
Peddibhotla S, Shi R, Khan P, Smith LH, Mangravita-Novo A, Vicchiarelli M, Su Y, Okolotowicz KJ, Cashman JR, Reed JC, Roth GP. Peddibhotla S, et al. Among authors: roth gp. J Med Chem. 2010 Jun 24;53(12):4793-7. doi: 10.1021/jm1000248. J Med Chem. 2010. PMID: 20481485 Free PMC article.
37 results