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Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor.
Yingling JM, McMillen WT, Yan L, Huang H, Sawyer JS, Graff J, Clawson DK, Britt KS, Anderson BD, Beight DW, Desaiah D, Lahn MM, Benhadji KA, Lallena MJ, Holmgaard RB, Xu X, Zhang F, Manro JR, Iversen PW, Iyer CV, Brekken RA, Kalos MD, Driscoll KE. Yingling JM, et al. Among authors: yan l. Oncotarget. 2017 Dec 31;9(6):6659-6677. doi: 10.18632/oncotarget.23795. eCollection 2018 Jan 23. Oncotarget. 2017. PMID: 29467918 Free PMC article.
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Sawyer JS, Anderson BD, Beight DW, Campbell RM, Jones ML, Herron DK, Lampe JW, McCowan JR, McMillen WT, Mort N, Parsons S, Smith EC, Vieth M, Weir LC, Yan L, Zhang F, Yingling JM. Sawyer JS, et al. Among authors: yan l. J Med Chem. 2003 Sep 11;46(19):3953-6. doi: 10.1021/jm0205705. J Med Chem. 2003. PMID: 12954047
Dihydropyrrolopyrazole transforming growth factor-beta type I receptor kinase domain inhibitors: a novel benzimidazole series with selectivity versus transforming growth factor-beta type II receptor kinase and mixed lineage kinase-7.
Li HY, Wang Y, Heap CR, King CH, Mundla SR, Voss M, Clawson DK, Yan L, Campbell RM, Anderson BD, Wagner JR, Britt K, Lu KX, McMillen WT, Yingling JM. Li HY, et al. Among authors: yan l. J Med Chem. 2006 Mar 23;49(6):2138-42. doi: 10.1021/jm058209g. J Med Chem. 2006. PMID: 16539403
Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent.
Li HY, McMillen WT, Heap CR, McCann DJ, Yan L, Campbell RM, Mundla SR, King CH, Dierks EA, Anderson BD, Britt KS, Huss KL, Voss MD, Wang Y, Clawson DK, Yingling JM, Sawyer JS. Li HY, et al. Among authors: yan l. J Med Chem. 2008 Apr 10;51(7):2302-6. doi: 10.1021/jm701199p. Epub 2008 Mar 4. J Med Chem. 2008. PMID: 18314943
Synthesis and activity of new aryl- and heteroaryl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
Sawyer JS, Beight DW, Britt KS, Anderson BD, Campbell RM, Goodson T Jr, Herron DK, Li HY, McMillen WT, Mort N, Parsons S, Smith EC, Wagner JR, Yan L, Zhang F, Yingling JM. Sawyer JS, et al. Among authors: yan l. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3581-4. doi: 10.1016/j.bmcl.2004.04.007. Bioorg Med Chem Lett. 2004. PMID: 15177479
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