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Page 1
Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development.
Sun D, Li Z, Rew Y, Gribble M, Bartberger MD, Beck HP, Canon J, Chen A, Chen X, Chow D, Deignan J, Duquette J, Eksterowicz J, Fisher B, Fox BM, Fu J, Gonzalez AZ, Gonzalez-Lopez De Turiso F, Houze JB, Huang X, Jiang M, Jin L, Kayser F, Liu JJ, Lo MC, Long AM, Lucas B, McGee LR, McIntosh J, Mihalic J, Oliner JD, Osgood T, Peterson ML, Roveto P, Saiki AY, Shaffer P, Toteva M, Wang Y, Wang YC, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Yu M, Zhao X, Zhou J, Zhu J, Olson SH, Medina JC. Sun D, et al. Among authors: deignan j. J Med Chem. 2014 Feb 27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5. J Med Chem. 2014. PMID: 24456472
Discovery of AMG 925, a FLT3 and CDK4 dual kinase inhibitor with preferential affinity for the activated state of FLT3.
Li Z, Wang X, Eksterowicz J, Gribble MW Jr, Alba GQ, Ayres M, Carlson TJ, Chen A, Chen X, Cho R, Connors RV, DeGraffenreid M, Deignan JT, Duquette J, Fan P, Fisher B, Fu J, Huard JN, Kaizerman J, Keegan KS, Li C, Li K, Li Y, Liang L, Liu W, Lively SE, Lo MC, Ma J, McMinn DL, Mihalic JT, Modi K, Ngo R, Pattabiraman K, Piper DE, Queva C, Ragains ML, Suchomel J, Thibault S, Walker N, Wang X, Wang Z, Wanska M, Wehn PM, Weidner MF, Zhang AJ, Zhao X, Kamb A, Wickramasinghe D, Dai K, McGee LR, Medina JC. Li Z, et al. Among authors: deignan jt. J Med Chem. 2014 Apr 24;57(8):3430-49. doi: 10.1021/jm500118j. Epub 2014 Apr 2. J Med Chem. 2014. PMID: 24641103
Structure-based design of novel inhibitors of the MDM2-p53 interaction.
Rew Y, Sun D, Gonzalez-Lopez De Turiso F, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Deignan J, Fox BM, Gustin D, Huang X, Jiang M, Jiao X, Jin L, Kayser F, Kopecky DJ, Li Y, Lo MC, Long AM, Michelsen K, Oliner JD, Osgood T, Ragains M, Saiki AY, Schneider S, Toteva M, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH. Rew Y, et al. Among authors: deignan j. J Med Chem. 2012 Jun 14;55(11):4936-54. doi: 10.1021/jm300354j. Epub 2012 May 9. J Med Chem. 2012. PMID: 22524527
Optimization beyond AMG 232: discovery and SAR of sulfonamides on a piperidinone scaffold as potent inhibitors of the MDM2-p53 protein-protein interaction.
Wang Y, Zhu J, Liu JJ, Chen X, Mihalic J, Deignan J, Yu M, Sun D, Kayser F, McGee LR, Lo MC, Chen A, Zhou J, Ye Q, Huang X, Long AM, Yakowec P, Oliner JD, Olson SH, Medina JC. Wang Y, et al. Among authors: deignan j. Bioorg Med Chem Lett. 2014 Aug 15;24(16):3782-5. doi: 10.1016/j.bmcl.2014.06.073. Epub 2014 Jul 1. Bioorg Med Chem Lett. 2014. PMID: 25042256
Discovery of potent and specific CXCR3 antagonists.
Chen X, Mihalic J, Deignan J, Gustin DJ, Duquette J, Du X, Chan J, Fu Z, Johnson M, Li AR, Henne K, Sullivan T, Lemon B, Ma J, Miao S, Tonn G, Collins T, Medina JC. Chen X, et al. Among authors: deignan j. Bioorg Med Chem Lett. 2012 Jan 1;22(1):357-62. doi: 10.1016/j.bmcl.2011.10.120. Epub 2011 Nov 9. Bioorg Med Chem Lett. 2012. PMID: 22130135
Discovery of a new class of ghrelin receptor antagonists.
Mihalic JT, Kim YJ, Lizarzaburu M, Chen X, Deignan J, Wanska M, Yu M, Fu J, Chen X, Zhang A, Connors R, Liang L, Lindstrom M, Ma J, Tang L, Dai K, Li L. Mihalic JT, et al. Among authors: deignan j. Bioorg Med Chem Lett. 2012 Mar 1;22(5):2046-51. doi: 10.1016/j.bmcl.2012.01.014. Epub 2012 Jan 14. Bioorg Med Chem Lett. 2012. PMID: 22305493
Structure-guided design, synthesis, and evaluation of guanine-derived inhibitors of the eIF4E mRNA-cap interaction.
Chen X, Kopecky DJ, Mihalic J, Jeffries S, Min X, Heath J, Deignan J, Lai S, Fu Z, Guimaraes C, Shen S, Li S, Johnstone S, Thibault S, Xu H, Cardozo M, Shen W, Walker N, Kayser F, Wang Z. Chen X, et al. Among authors: deignan j. J Med Chem. 2012 Apr 26;55(8):3837-51. doi: 10.1021/jm300037x. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22458568
Optimization of the heterocyclic core of the quinazolinone-derived CXCR3 antagonists.
Li AR, Johnson MG, Liu J, Chen X, Du X, Mihalic JT, Deignan J, Gustin DJ, Duquette J, Fu Z, Zhu L, Marcus AP, Bergeron P, McGee LR, Danao J, Lemon B, Carabeo T, Sullivan T, Ma J, Tang L, Tonn G, Collins TL, Medina JC. Li AR, et al. Among authors: deignan j. Bioorg Med Chem Lett. 2008 Jan 15;18(2):688-93. doi: 10.1016/j.bmcl.2007.11.060. Epub 2007 Nov 21. Bioorg Med Chem Lett. 2008. PMID: 18061451
Design and optimization of imidazole derivatives as potent CXCR3 antagonists.
Du X, Chen X, Mihalic JT, Deignan J, Duquette J, Li AR, Lemon B, Ma J, Miao S, Ebsworth K, Sullivan TJ, Tonn G, Collins TL, Medina JC. Du X, et al. Among authors: deignan j. Bioorg Med Chem Lett. 2008 Jan 15;18(2):608-13. doi: 10.1016/j.bmcl.2007.11.072. Epub 2007 Nov 28. Bioorg Med Chem Lett. 2008. PMID: 18063364
73 results