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Page 1
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: pullen ss. 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, 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: pullen ss. 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
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: pullen ss. 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: pullen ss. 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
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. Riether D, et al. Among authors: pullen ss. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1588-91. doi: 10.1016/j.bmcl.2009.02.012. Epub 2009 Feb 8. Bioorg Med Chem Lett. 2009. PMID: 19246196
Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region.
Lo HY, Nemoto PA, Kim JM, Hao MH, Qian KC, Farrow NA, Albaugh DR, Fowler DM, Schneiderman RD, Michael August E, Martin L, Hill-Drzewi M, Pullen SS, Takahashi H, De Lombaert S. Lo HY, et al. Among authors: pullen ss. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4533-9. doi: 10.1016/j.bmcl.2011.05.126. Epub 2011 Jun 17. Bioorg Med Chem Lett. 2011. PMID: 21733690
Three mechanistically distinct kinase assays compared: Measurement of intrinsic ATPase activity identified the most comprehensive set of ITK inhibitors.
Kashem MA, Nelson RM, Yingling JD, Pullen SS, Prokopowicz AS 3rd, Jones JW, Wolak JP, Rogers GR, Morelock MM, Snow RJ, Homon CA, Jakes S. Kashem MA, et al. Among authors: pullen ss. J Biomol Screen. 2007 Feb;12(1):70-83. doi: 10.1177/1087057106296047. Epub 2006 Dec 8. J Biomol Screen. 2007. PMID: 17166826
Discovery of potent, selective chymase inhibitors via fragment linking strategies.
Taylor SJ, Padyana AK, Abeywardane A, Liang S, Hao MH, De Lombaert S, Proudfoot J, Farmer BS 3rd, Li X, Collins B, Martin L, Albaugh DR, Hill-Drzewi M, Pullen SS, Takahashi H. Taylor SJ, et al. Among authors: pullen ss. J Med Chem. 2013 Jun 13;56(11):4465-81. doi: 10.1021/jm400138z. Epub 2013 Jun 4. J Med Chem. 2013. PMID: 23659209
36 results