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Heteroarylamide smoothened inhibitors: Discovery of N-[2,4-dimethyl-5-(1-methylimidazol-4-yl)phenyl]-4-(2-pyridylmethoxy)benzamide (AZD8542) and N-[5-(1H-imidazol-2-yl)-2,4-dimethyl-phenyl]-4-(2- pyridylmethoxy)benzamide (AZD7254).
Yang B, Hird AW, Bodnarchuk MS, Zheng X, Dakin L, Su Q, Daly K, Godin R, Hattersley MM, Brassil P, Redmond S, John Russell D, Janetka JW. Yang B, et al. Among authors: janetka jw. Bioorg Med Chem. 2020 Jan 15;28(2):115227. doi: 10.1016/j.bmc.2019.115227. Epub 2019 Dec 11. Bioorg Med Chem. 2020. PMID: 31862310
Discovery of a novel class of 2-ureido thiophene carboxamide checkpoint kinase inhibitors.
Janetka JW, Almeida L, Ashwell S, Brassil PJ, Daly K, Deng C, Gero T, Glynn RE, Horn CL, Ioannidis S, Lyne P, Newcombe NJ, Oza VB, Pass M, Springer SK, Su M, Toader D, Vasbinder MM, Yu D, Yu Y, Zabludoff SD. Janetka JW, et al. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4242-8. doi: 10.1016/j.bmcl.2008.05.016. Epub 2008 May 6. Bioorg Med Chem Lett. 2008. PMID: 18547806
Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.
Oza V, Ashwell S, Brassil P, Breed J, Deng C, Ezhuthachan J, Haye H, Horn C, Janetka J, Lyne P, Newcombe N, Otterbien L, Pass M, Read J, Roswell S, Su M, Toader D, Yu D, Yu Y, Valentine A, Webborn P, White A, Zabludoff S, Zheng X. Oza V, et al. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5133-8. doi: 10.1016/j.bmcl.2010.07.015. Epub 2010 Jul 29. Bioorg Med Chem Lett. 2010. PMID: 20673630
Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.
Oza V, Ashwell S, Almeida L, Brassil P, Breed J, Deng C, Gero T, Grondine M, Horn C, Ioannidis S, Liu D, Lyne P, Newcombe N, Pass M, Read J, Ready S, Rowsell S, Su M, Toader D, Vasbinder M, Yu D, Yu Y, Xue Y, Zabludoff S, Janetka J. Oza V, et al. J Med Chem. 2012 Jun 14;55(11):5130-42. doi: 10.1021/jm300025r. Epub 2012 Jun 4. J Med Chem. 2012. PMID: 22551018
Diaryldimethylpiperazine ligands with mu- and delta-opioid receptor affinity: Synthesis of (+)-4-[(alphaR)-alpha-(4-allyl-(2S,5S)-dimethylpiperazin-1-yl)-(3-hydroxyphenyl)methyl]-N-ethyl-N-phenylbenzamide and (-)-4-[(alphaR)-alpha-(2S,5S)-dimethylpiperazin-1-yl)-(3-hydroxyphenyl)methyl]-N-ethyl-N-phenylbenzamide.
Kim IJ, Ullrich T, Janetka JW, Furness MS, Jacobson AE, Rothman RB, Dersch CM, Flippen-Anderson JL, George C, Rice KC. Kim IJ, et al. Among authors: janetka jw. Bioorg Med Chem. 2003 Nov 3;11(22):4761-8. doi: 10.1016/s0968-0896(03)00496-6. Bioorg Med Chem. 2003. PMID: 14556791
Flipped out: structure-guided design of selective pyrazolylpyrrole ERK inhibitors.
Aronov AM, Baker C, Bemis GW, Cao J, Chen G, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Martinez-Botella G, Namchuk MN, Straub J, Tang Q, Xie X. Aronov AM, et al. Among authors: janetka jw. J Med Chem. 2007 Mar 22;50(6):1280-7. doi: 10.1021/jm061381f. Epub 2007 Feb 15. J Med Chem. 2007. PMID: 17300186
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.
Aronov AM, Tang Q, Martinez-Botella G, Bemis GW, Cao J, Chen G, Ewing NP, Ford PJ, Germann UA, Green J, Hale MR, Jacobs M, Janetka JW, Maltais F, Markland W, Namchuk MN, Nanthakumar S, Poondru S, Straub J, ter Haar E, Xie X. Aronov AM, et al. Among authors: janetka jw. J Med Chem. 2009 Oct 22;52(20):6362-8. doi: 10.1021/jm900630q. J Med Chem. 2009. PMID: 19827834
65 results