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Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N. Chu XJ, et al. Among authors: depinto w. J Med Chem. 2006 Nov 2;49(22):6549-60. doi: 10.1021/jm0606138. J Med Chem. 2006. PMID: 17064073
3,5,6-Trisubstituted naphthostyrils as CDK2 inhibitors.
Liu JJ, Dermatakis A, Lukacs C, Konzelmann F, Chen Y, Kammlott U, Depinto W, Yang H, Yin X, Chen Y, Schutt A, Simcox ME, Luk KC. Liu JJ, et al. Among authors: depinto w. Bioorg Med Chem Lett. 2003 Aug 4;13(15):2465-8. doi: 10.1016/s0960-894x(03)00488-8. Bioorg Med Chem Lett. 2003. PMID: 12852944
In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials.
DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R, Xiang Q, Tovar C, Blain R, Nevins T, Higgins B, Luistro L, Kolinsky K, Felix B, Hussain S, Heimbrook D. DePinto W, et al. Mol Cancer Ther. 2006 Nov;5(11):2644-58. doi: 10.1158/1535-7163.MCT-06-0355. Mol Cancer Ther. 2006. PMID: 17121911
Synthesis of potent oxindole CDK2 inhibitors.
Dermatakis A, Luk KC, DePinto W. Dermatakis A, et al. Among authors: depinto w. Bioorg Med Chem. 2003 Apr 17;11(8):1873-81. doi: 10.1016/s0968-0896(03)00036-1. Bioorg Med Chem. 2003. PMID: 12659774
A new series of potent oxindole inhibitors of CDK2.
Luk KC, Simcox ME, Schutt A, Rowan K, Thompson T, Chen Y, Kammlott U, DePinto W, Dunten P, Dermatakis A. Luk KC, et al. Among authors: depinto w. Bioorg Med Chem Lett. 2004 Feb 23;14(4):913-7. doi: 10.1016/j.bmcl.2003.12.009. Bioorg Med Chem Lett. 2004. PMID: 15012993
Preclinical biomarkers for a cyclin-dependent kinase inhibitor translate to candidate pharmacodynamic biomarkers in phase I patients.
Berkofsky-Fessler W, Nguyen TQ, Delmar P, Molnos J, Kanwal C, DePinto W, Rosinski J, McLoughlin P, Ritland S, DeMario M, Tobon K, Reidhaar-Olson JF, Rueger R, Hilton H. Berkofsky-Fessler W, et al. Among authors: depinto w. Mol Cancer Ther. 2009 Sep;8(9):2517-25. doi: 10.1158/1535-7163.MCT-09-0083. Epub 2009 Sep 15. Mol Cancer Ther. 2009. PMID: 19755512 Clinical Trial.
Inhibition of S/G2 phase CDK4 reduces mitotic fidelity.
Burgess A, Wigan M, Giles N, Depinto W, Gillespie P, Stevens F, Gabrielli B. Burgess A, et al. Among authors: depinto w. J Biol Chem. 2006 Apr 14;281(15):9987-95. doi: 10.1074/jbc.M512714200. Epub 2006 Feb 13. J Biol Chem. 2006. PMID: 16476733 Free article.