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Page 1
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: packman k. J Med Chem. 2006 Nov 2;49(22):6549-60. doi: 10.1021/jm0606138. J Med Chem. 2006. PMID: 17064073
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. Among authors: packman k. Mol Cancer Ther. 2006 Nov;5(11):2644-58. doi: 10.1158/1535-7163.MCT-06-0355. Mol Cancer Ther. 2006. PMID: 17121911
Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development.
Ding Q, Zhang Z, Liu JJ, Jiang N, Zhang J, Ross TM, Chu XJ, Bartkovitz D, Podlaski F, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B. Ding Q, et al. Among authors: packman k. J Med Chem. 2013 Jul 25;56(14):5979-83. doi: 10.1021/jm400487c. Epub 2013 Jul 16. J Med Chem. 2013. PMID: 23808545
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
Vu B, Wovkulich P, Pizzolato G, Lovey A, Ding Q, Jiang N, Liu JJ, Zhao C, Glenn K, Wen Y, Tovar C, Packman K, Vassilev L, Graves B. Vu B, et al. Among authors: packman k. ACS Med Chem Lett. 2013 Apr 2;4(5):466-9. doi: 10.1021/ml4000657. eCollection 2013 May 9. ACS Med Chem Lett. 2013. PMID: 24900694 Free PMC article.
Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.
Zhang Z, Chu XJ, Liu JJ, Ding Q, Zhang J, Bartkovitz D, Jiang N, Karnachi P, So SS, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev L, Graves B. Zhang Z, et al. Among authors: packman k. ACS Med Chem Lett. 2013 Dec 29;5(2):124-7. doi: 10.1021/ml400359z. eCollection 2014 Feb 13. ACS Med Chem Lett. 2013. PMID: 24900784 Free PMC article.
Characterization of a novel mitogen-activated protein kinase kinase 1/2 inhibitor with a unique mechanism of action for cancer therapy.
Daouti S, Wang H, Li WH, Higgins B, Kolinsky K, Packman K, Specian A Jr, Kong N, Huby N, Wen Y, Xiang Q, Podlaski FJ, He Y, Fotouhi N, Heimbrook D, Niu H. Daouti S, et al. Among authors: packman k. Cancer Res. 2009 Mar 1;69(5):1924-32. doi: 10.1158/0008-5472.CAN-08-2627. Epub 2009 Feb 24. Cancer Res. 2009. PMID: 19244124
Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models.
Daouti S, Higgins B, Kolinsky K, Packman K, Wang H, Rizzo C, Moliterni J, Huby N, Fotouhi N, Liu M, Goelzer P, Sandhu HK, Li JK, Railkar A, Heimbrook D, Niu H. Daouti S, et al. Among authors: packman k. Mol Cancer Ther. 2010 Jan;9(1):134-44. doi: 10.1158/1535-7163.MCT-09-0601. Epub 2010 Jan 6. Mol Cancer Ther. 2010. PMID: 20053779
52 results