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Page 1
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Harris CM, Ericsson AM, Argiriadi MA, Barberis C, Borhani DW, Burchat A, Calderwood DJ, Cunha GA, Dixon RW, Frank KE, Johnson EF, Kamens J, Kwak S, Li B, Mullen KD, Perron DC, Wang L, Wishart N, Wu X, Zhang X, Zmetra TR, Talanian RV. Harris CM, et al. Among authors: cunha ga. Bioorg Med Chem Lett. 2010 Jan 1;20(1):334-7. doi: 10.1016/j.bmcl.2009.10.103. Epub 2009 Oct 29. Bioorg Med Chem Lett. 2010. PMID: 19926477
Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors.
Dinges J, Akritopoulou-Zanze I, Arnold LD, Barlozzari T, Bousquet PF, Cunha GA, Ericsson AM, Iwasaki N, Michaelides MR, Ogawa N, Phelan KM, Rafferty P, Sowin TJ, Stewart KD, Tokuyama R, Xia Z, Zhang HQ. Dinges J, et al. Among authors: cunha ga. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4371-5. doi: 10.1016/j.bmcl.2006.05.052. Epub 2006 Jun 5. Bioorg Med Chem Lett. 2006. PMID: 16750628
Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor.
Dai Y, Hartandi K, Ji Z, Ahmed AA, Albert DH, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Harris CM, Hickman D, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Martin RL, Olson AM, Osterling DJ, Pease LJ, Soni NB, Stewart KD, Stoll VS, Tapang P, Reuter DR, Davidsen SK, Michaelides MR. Dai Y, et al. Among authors: cunha ga. J Med Chem. 2007 Apr 5;50(7):1584-97. doi: 10.1021/jm061280h. Epub 2007 Mar 8. J Med Chem. 2007. PMID: 17343372
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.
Dinges J, Albert DH, Arnold LD, Ashworth KL, Akritopoulou-Zanze I, Bousquet PF, Bouska JJ, Cunha GA, Davidsen SK, Diaz GJ, Djuric SW, Gasiecki AF, Gintant GA, Gracias VJ, Harris CM, Houseman KA, Hutchins CW, Johnson EF, Li H, Marcotte PA, Martin RL, Michaelides MR, Nyein M, Sowin TJ, Su Z, Tapang PH, Xia Z, Zhang HQ. Dinges J, et al. Among authors: cunha ga. J Med Chem. 2007 May 3;50(9):2011-29. doi: 10.1021/jm061223o. Epub 2007 Apr 11. J Med Chem. 2007. PMID: 17425296
3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.
Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Diaz G, Glaser KB, Guo J, Harris CM, Li J, Marcotte PA, Moskey MD, Oie T, Pease L, Soni NB, Stewart KD, Davidsen SK, Michaelides MR. Ji Z, et al. Among authors: cunha ga. J Med Chem. 2008 Mar 13;51(5):1231-41. doi: 10.1021/jm701096v. Epub 2008 Feb 9. J Med Chem. 2008. PMID: 18260617
Thienopyrimidine ureas as novel and potent multitargeted receptor tyrosine kinase inhibitors.
Dai Y, Guo Y, Frey RR, Ji Z, Curtin ML, Ahmed AA, Albert DH, Arnold L, Arries SS, Barlozzari T, Bauch JL, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Marsh KC, Moskey MD, Pease LJ, Stewart KD, Stoll VS, Tapang P, Wishart N, Davidsen SK, Michaelides MR. Dai Y, et al. Among authors: cunha ga. J Med Chem. 2005 Sep 22;48(19):6066-83. doi: 10.1021/jm050458h. J Med Chem. 2005. PMID: 16162008
Isothiazolopyrimidines and isoxazolopyrimidines as novel multi-targeted inhibitors of receptor tyrosine kinases.
Ji Z, Ahmed AA, Albert DH, Bouska JJ, Bousquet PF, Cunha GA, Glaser KB, Guo J, Li J, Marcotte PA, Moskey MD, Pease LJ, Stewart KD, Yates M, Davidsen SK, Michaelides MR. Ji Z, et al. Among authors: cunha ga. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4326-30. doi: 10.1016/j.bmcl.2006.05.057. Epub 2006 Jun 2. Bioorg Med Chem Lett. 2006. PMID: 16735117
Thienopyridine urea inhibitors of KDR kinase.
Heyman HR, Frey RR, Bousquet PF, Cunha GA, Moskey MD, Ahmed AA, Soni NB, Marcotte PA, Pease LJ, Glaser KB, Yates M, Bouska JJ, Albert DH, Black-Schaefer CL, Dandliker PJ, Stewart KD, Rafferty P, Davidsen SK, Michaelides MR, Curtin ML. Heyman HR, et al. Among authors: cunha ga. Bioorg Med Chem Lett. 2007 Mar 1;17(5):1246-9. doi: 10.1016/j.bmcl.2006.12.015. Epub 2006 Dec 9. Bioorg Med Chem Lett. 2007. PMID: 17188869
Isoindolinone ureas: a novel class of KDR kinase inhibitors.
Curtin ML, Frey RR, Heyman HR, Sarris KA, Steinman DH, Holmes JH, Bousquet PF, Cunha GA, Moskey MD, Ahmed AA, Pease LJ, Glaser KB, Stewart KD, Davidsen SK, Michaelides MR. Curtin ML, et al. Among authors: cunha ga. Bioorg Med Chem Lett. 2004 Sep 6;14(17):4505-9. doi: 10.1016/j.bmcl.2004.06.041. Bioorg Med Chem Lett. 2004. PMID: 15357981
15 results