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Page 1
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Gommermann N, Buehlmayer P, von Matt A, Breitenstein W, Masuya K, Pirard B, Furet P, Cowan-Jacob SW, Weckbecker G. Gommermann N, et al. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3628-31. doi: 10.1016/j.bmcl.2010.04.112. Epub 2010 Apr 29. Bioorg Med Chem Lett. 2010. PMID: 20483608
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.
Karpov AS, Amiri P, Bellamacina C, Bellance MH, Breitenstein W, Daniel D, Denay R, Fabbro D, Fernandez C, Galuba I, Guerro-Lagasse S, Gutmann S, Hinh L, Jahnke W, Klopp J, Lai A, Lindvall MK, Ma S, Möbitz H, Pecchi S, Rummel G, Shoemaker K, Trappe J, Voliva C, Cowan-Jacob SW, Marzinzik AL. Karpov AS, et al. Among authors: cowan jacob sw. ACS Med Chem Lett. 2015 May 22;6(7):776-81. doi: 10.1021/acsmedchemlett.5b00102. eCollection 2015 Jul 9. ACS Med Chem Lett. 2015. PMID: 26191365 Free PMC article.
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Schoepfer J, Jahnke W, Berellini G, Buonamici S, Cotesta S, Cowan-Jacob SW, Dodd S, Drueckes P, Fabbro D, Gabriel T, Groell JM, Grotzfeld RM, Hassan AQ, Henry C, Iyer V, Jones D, Lombardo F, Loo A, Manley PW, Pellé X, Rummel G, Salem B, Warmuth M, Wylie AA, Zoller T, Marzinzik AL, Furet P. Schoepfer J, et al. Among authors: cowan jacob sw. J Med Chem. 2018 Sep 27;61(18):8120-8135. doi: 10.1021/acs.jmedchem.8b01040. Epub 2018 Sep 7. J Med Chem. 2018. PMID: 30137981
Expanding the diversity of allosteric bcr-abl inhibitors.
Deng X, Okram B, Ding Q, Zhang J, Choi Y, Adrián FJ, Wojciechowski A, Zhang G, Che J, Bursulaya B, Cowan-Jacob SW, Rummel G, Sim T, Gray NS. Deng X, et al. J Med Chem. 2010 Oct 14;53(19):6934-46. doi: 10.1021/jm100555f. J Med Chem. 2010. PMID: 20828158 Free PMC article.
Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site.
Fabbro D, Manley PW, Jahnke W, Liebetanz J, Szyttenholm A, Fendrich G, Strauss A, Zhang J, Gray NS, Adrian F, Warmuth M, Pelle X, Grotzfeld R, Berst F, Marzinzik A, Cowan-Jacob SW, Furet P, Mestan J. Fabbro D, et al. Biochim Biophys Acta. 2010 Mar;1804(3):454-62. doi: 10.1016/j.bbapap.2009.12.009. Biochim Biophys Acta. 2010. PMID: 20152788
Imidazo[1,2-a]pyridin-6-yl-benzamide analogs as potent RAF inhibitors.
Smith A, Ni ZJ, Poon D, Huang Z, Chen Z, Zhang Q, Tandeske L, Merritt H, Shoemaker K, Chan J, Kaufman S, Huh K, Murray J, Appleton BA, Cowan-Jacob SW, Scheufler C, Kanazawa T, Jansen JM, Stuart D, Shafer CM. Smith A, et al. Among authors: cowan jacob sw. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5221-5224. doi: 10.1016/j.bmcl.2017.10.047. Epub 2017 Oct 20. Bioorg Med Chem Lett. 2017. PMID: 29107542
49 results