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2-Anilino-4-aryl-1,3-thiazole inhibitors of valosin-containing protein (VCP or p97).
Bursavich MG, Parker DP, Willardsen JA, Gao ZH, Davis T, Ostanin K, Robinson R, Peterson A, Cimbora DM, Zhu JF, Richards B. Bursavich MG, et al. Among authors: willardsen ja. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1677-9. doi: 10.1016/j.bmcl.2010.01.058. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20137940
Analogues of 4-[(7-Bromo-2-methyl-4-oxo-3H-quinazolin-6-yl)methylprop-2-ynylamino]-N-(3-pyridylmethyl)benzamide (CB-30865) as potent inhibitors of nicotinamide phosphoribosyltransferase (Nampt).
Lockman JW, Murphy BR, Zigar DF, Judd WR, Slattum PM, Gao ZH, Ostanin K, Green J, McKinnon R, Terry-Lorenzo RT, Fleischer TC, Boniface JJ, Shenderovich M, Willardsen JA. Lockman JW, et al. Among authors: willardsen ja. J Med Chem. 2010 Dec 23;53(24):8734-46. doi: 10.1021/jm101145b. Epub 2010 Nov 16. J Med Chem. 2010. PMID: 21080724
Characterization of the cellular and antitumor effects of MPI-0479605, a small-molecule inhibitor of the mitotic kinase Mps1.
Tardif KD, Rogers A, Cassiano J, Roth BL, Cimbora DM, McKinnon R, Peterson A, Douce TB, Robinson R, Dorweiler I, Davis T, Hess MA, Ostanin K, Papac DI, Baichwal V, McAlexander I, Willardsen JA, Saunders M, Christophe H, Kumar DV, Wettstein DA, Carlson RO, Williams BL. Tardif KD, et al. Among authors: willardsen ja. Mol Cancer Ther. 2011 Dec;10(12):2267-75. doi: 10.1158/1535-7163.MCT-11-0453. Epub 2011 Oct 6. Mol Cancer Ther. 2011. PMID: 21980130
Discovery of 2-chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a potent inducer of apoptosis with high in vivo activity.
Sirisoma N, Kasibhatla S, Pervin A, Zhang H, Jiang S, Willardsen JA, Anderson MB, Baichwal V, Mather GG, Jessing K, Hussain R, Hoang K, Pleiman CM, Tseng B, Drewe J, Cai SX. Sirisoma N, et al. Among authors: willardsen ja. J Med Chem. 2008 Aug 14;51(15):4771-9. doi: 10.1021/jm8003653. Epub 2008 Jul 24. J Med Chem. 2008. PMID: 18651728
Oxindole derivatives as inhibitors of TAK1 kinase.
Lockman JW, Reeder MD, Robinson R, Ormonde PA, Cimbora DM, Williams BL, Willardsen JA. Lockman JW, et al. Among authors: willardsen ja. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1724-7. doi: 10.1016/j.bmcl.2011.01.077. Epub 2011 Jan 26. Bioorg Med Chem Lett. 2011. PMID: 21316225
The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2.
Kohrt JT, Filipski KJ, Cody WL, Cai C, Dudley DA, Van Huis CA, Willardsen JA, Narasimhan LS, Zhang E, Rapundalo ST, Saiya-Cork K, Leadley RJ, Edmunds JJ. Kohrt JT, et al. Among authors: willardsen ja. Bioorg Med Chem Lett. 2006 Feb 15;16(4):1060-4. doi: 10.1016/j.bmcl.2005.10.076. Epub 2005 Nov 11. Bioorg Med Chem Lett. 2006. PMID: 16289811
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