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2-Amino-aryl-7-aryl-benzoxazoles as potent, selective and orally available JAK2 inhibitors.
Gerspacher M, Furet P, Pissot-Soldermann C, Gaul C, Holzer P, Vangrevelinghe E, Lang M, Erdmann D, Radimerski T, Regnier CH, Chene P, De Pover A, Hofmann F, Baffert F, Buhl T, Aichholz R, Blasco F, Endres R, Trappe J, Drueckes P. Gerspacher M, et al. Among authors: lang m. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1724-7. doi: 10.1016/j.bmcl.2010.01.069. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20138510
Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805.
Baffert F, Régnier CH, De Pover A, Pissot-Soldermann C, Tavares GA, Blasco F, Brueggen J, Chène P, Drueckes P, Erdmann D, Furet P, Gerspacher M, Lang M, Ledieu D, Nolan L, Ruetz S, Trappe J, Vangrevelinghe E, Wartmann M, Wyder L, Hofmann F, Radimerski T. Baffert F, et al. Among authors: lang m. Mol Cancer Ther. 2010 Jul;9(7):1945-55. doi: 10.1158/1535-7163.MCT-10-0053. Epub 2010 Jun 29. Mol Cancer Ther. 2010. PMID: 20587663
Debio 0617B Inhibits Growth of STAT3-Driven Solid Tumors through Combined Inhibition of JAK, SRC, and Class III/V Receptor Tyrosine Kinases.
Murone M, Vaslin Chessex A, Attinger A, Ramachandra R, Shetty SJ, Daginakatte G, Sengupta S, Marappan S, Dhodheri S, Rigotti S, Bachhav Y, Brienza S, Traxler P, Lang M, Aguet M, Zoete V, Michielin O, Nicholas C, Johnson FM, Ramachandra M, McAllister A. Murone M, et al. Among authors: lang m. Mol Cancer Ther. 2016 Oct;15(10):2334-2343. doi: 10.1158/1535-7163.MCT-15-0974. Epub 2016 Jul 20. Mol Cancer Ther. 2016. PMID: 27439479