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Items: 1 to 20 of 132

1.

Novel inhibitors of the MDM2-p53 interaction featuring hydrogen bond acceptors as carboxylic acid isosteres.

Gonzalez AZ, Li Z, Beck HP, Canon J, Chen A, Chow D, Duquette J, Eksterowicz J, Fox BM, Fu J, Huang X, Houze J, Jin L, Li Y, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Sun D, Medina JC.

J Med Chem. 2014 Apr 10;57(7):2963-88. doi: 10.1021/jm401911v. Epub 2014 Mar 27.

PMID:
24601644
2.

Selective and potent morpholinone inhibitors of the MDM2-p53 protein-protein interaction.

Gonzalez AZ, Eksterowicz J, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Duquette J, Fox BM, Fu J, Huang X, Houze JB, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, McMinn DL, Oliner JD, Osgood T, Rew Y, Saiki AY, Shaffer P, Wortman S, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Olson SH, Medina JC, Sun D.

J Med Chem. 2014 Mar 27;57(6):2472-88. doi: 10.1021/jm401767k. Epub 2014 Mar 4.

PMID:
24548297
3.

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.

J Med Chem. 2014 Feb 27;57(4):1454-72. doi: 10.1021/jm401753e. Epub 2014 Feb 5.

PMID:
24456472
4.

Discovery of AM-7209, a potent and selective 4-amidobenzoic acid inhibitor of the MDM2-p53 interaction.

Rew Y, Sun D, Yan X, Beck HP, Canon J, Chen A, Duquette J, Eksterowicz J, Fox BM, Fu J, Gonzalez AZ, Houze J, Huang X, Jiang M, Jin L, Li Y, Li Z, Ling Y, Lo MC, Long AM, McGee LR, McIntosh J, Oliner JD, Osgood T, Saiki AY, Shaffer P, Wang YC, Wortman S, Yakowec P, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH.

J Med Chem. 2014 Dec 26;57(24):10499-511. doi: 10.1021/jm501550p. Epub 2014 Dec 4.

PMID:
25384157
5.

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.

J Med Chem. 2012 Jun 14;55(11):4936-54. doi: 10.1021/jm300354j. Epub 2012 May 9.

PMID:
22524527
6.

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.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3782-5. doi: 10.1016/j.bmcl.2014.06.073. Epub 2014 Jul 1.

PMID:
25042256
7.

Rational design and binding mode duality of MDM2-p53 inhibitors.

Gonzalez-Lopez de Turiso F, Sun D, Rew Y, Bartberger MD, Beck HP, Canon J, Chen A, Chow D, Correll TL, Huang X, Julian LD, Kayser F, Lo MC, Long AM, McMinn D, Oliner JD, Osgood T, Powers JP, Saiki AY, Schneider S, Shaffer P, Xiao SH, Yakowec P, Yan X, Ye Q, Yu D, Zhao X, Zhou J, Medina JC, Olson SH.

J Med Chem. 2013 May 23;56(10):4053-70. doi: 10.1021/jm400293z. Epub 2013 May 6.

PMID:
23597064
8.

Discovery, synthesis, and biological evaluation of orally active pyrrolidone derivatives as novel inhibitors of p53-MDM2 protein-protein interaction.

Zhuang C, Miao Z, Zhu L, Dong G, Guo Z, Wang S, Zhang Y, Wu Y, Yao J, Sheng C, Zhang W.

J Med Chem. 2012 Nov 26;55(22):9630-42. doi: 10.1021/jm300969t. Epub 2012 Oct 19.

PMID:
23046248
9.

The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents.

Canon J, Osgood T, Olson SH, Saiki AY, Robertson R, Yu D, Eksterowicz J, Ye Q, Jin L, Chen A, Zhou J, Cordover D, Kaufman S, Kendall R, Oliner JD, Coxon A, Radinsky R.

Mol Cancer Ther. 2015 Mar;14(3):649-58. doi: 10.1158/1535-7163.MCT-14-0710. Epub 2015 Jan 7.

10.

Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer.

Rew Y, Sun D.

J Med Chem. 2014 Aug 14;57(15):6332-41. doi: 10.1021/jm500627s. Epub 2014 Jul 9. Review.

PMID:
24967612
11.

Discovery of DS-5272 as a promising candidate: A potent and orally active p53-MDM2 interaction inhibitor.

Miyazaki M, Uoto K, Sugimoto Y, Naito H, Yoshida K, Okayama T, Kawato H, Miyazaki M, Kitagawa M, Seki T, Fukutake S, Aonuma M, Soga T.

Bioorg Med Chem. 2015 May 15;23(10):2360-7. doi: 10.1016/j.bmc.2015.03.069. Epub 2015 Mar 31.

PMID:
25882531
12.

Potent and orally active small-molecule inhibitors of the MDM2-p53 interaction.

Yu S, Qin D, Shangary S, Chen J, Wang G, Ding K, McEachern D, Qiu S, Nikolovska-Coleska Z, Miller R, Kang S, Yang D, Wang S.

J Med Chem. 2009 Dec 24;52(24):7970-3. doi: 10.1021/jm901400z.

13.

Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors.

Hu C, Li X, Wang W, Zhang L, Tao L, Dong X, Sheng R, Yang B, Hu Y.

Bioorg Med Chem. 2011 Sep 15;19(18):5454-61. doi: 10.1016/j.bmc.2011.07.050. Epub 2011 Jul 30.

PMID:
21855354
14.

Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency.

Hardcastle IR, Liu J, Valeur E, Watson A, Ahmed SU, Blackburn TJ, Bennaceur K, Clegg W, Drummond C, Endicott JA, Golding BT, Griffin RJ, Gruber J, Haggerty K, Harrington RW, Hutton C, Kemp S, Lu X, McDonnell JM, Newell DR, Noble ME, Payne SL, Revill CH, Riedinger C, Xu Q, Lunec J.

J Med Chem. 2011 Mar 10;54(5):1233-43. doi: 10.1021/jm1011929. Epub 2011 Feb 11.

PMID:
21314128
15.

A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.

Zhao Y, Yu S, Sun W, Liu L, Lu J, McEachern D, Shargary S, Bernard D, Li X, Zhao T, Zou P, Sun D, Wang S.

J Med Chem. 2013 Jul 11;56(13):5553-61. doi: 10.1021/jm4005708. Epub 2013 Jun 20.

16.

An expeditious synthesis of the MDM2-p53 inhibitor AM-8553.

Lucas BS, Fisher B, McGee LR, Olson SH, Medina JC, Cheung E.

J Am Chem Soc. 2012 Aug 1;134(30):12855-60. doi: 10.1021/ja305123v. Epub 2012 Jul 16.

PMID:
22734631
17.

Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein-protein interaction through structure-based drug design.

Parks DJ, LaFrance LV, Calvo RR, Milkiewicz KL, Marugán JJ, Raboisson P, Schubert C, Koblish HK, Zhao S, Franks CF, Lattanze J, Carver TE, Cummings MD, Maguire D, Grasberger BL, Maroney AC, Lu T.

Bioorg Med Chem Lett. 2006 Jun 15;16(12):3310-4. Epub 2006 Apr 4.

PMID:
16600594
18.
19.

Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannich ring-opening-cyclization reaction mechanism in spiro-oxindoles.

Aguilar A, Sun W, Liu L, Lu J, McEachern D, Bernard D, Deschamps JR, Wang S.

J Med Chem. 2014 Dec 26;57(24):10486-98. doi: 10.1021/jm501541j. Epub 2014 Dec 12.

20.

Small Molecule Inhibition of MDM2-p53 Interaction Augments Radiation Response in Human Tumors.

Werner LR, Huang S, Francis DM, Armstrong EA, Ma F, Li C, Iyer G, Canon J, Harari PM.

Mol Cancer Ther. 2015 Sep;14(9):1994-2003. doi: 10.1158/1535-7163.MCT-14-1056-T. Epub 2015 Jul 10.

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