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Items: 1 to 20 of 117

1.

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
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.

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
4.

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
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.

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
7.

Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors.

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

Bioorg Med Chem. 2013 Jul 15;21(14):4319-31. doi: 10.1016/j.bmc.2013.04.056. Epub 2013 Apr 30.

PMID:
23685175
8.

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
9.

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
10.

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
11.

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.

12.

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
13.

Design, synthesis and biological evaluation of novel 3,4,5-trisubstituted aminothiophenes as inhibitors of p53-MDM2 interaction. Part 2.

Wang W, Lv D, Qiu N, Zhang L, Hu C, Hu Y.

Bioorg Med Chem. 2013 Jun 1;21(11):2886-94. doi: 10.1016/j.bmc.2013.03.070. Epub 2013 Apr 6.

PMID:
23611770
14.

Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors.

Holzer P, Masuya K, Furet P, Kallen J, Valat-Stachyra T, Ferretti S, Berghausen J, Bouisset-Leonard M, Buschmann N, Pissot-Soldermann C, Rynn C, Ruetz S, Stutz S, Chène P, Jeay S, Gessier F.

J Med Chem. 2015 Aug 27;58(16):6348-58. doi: 10.1021/acs.jmedchem.5b00810. Epub 2015 Aug 5.

PMID:
26181851
15.

Design, synthesis and biological evaluation of novel potent MDM2/p53 small-molecule inhibitors.

Ivanenkov YA, Vasilevski SV, Beloglazkina EK, Kukushkin ME, Machulkin AE, Veselov MS, Chufarova NV, Chernyaginab ES, Vanzcool AS, Zyk NV, Skvortsov DA, Khutornenko AA, Rusanov AL, Tonevitsky AG, Dontsova OA, Majouga AG.

Bioorg Med Chem Lett. 2015 Jan 15;25(2):404-9. doi: 10.1016/j.bmcl.2014.09.070. Epub 2014 Oct 2.

PMID:
25479770
16.

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
17.

Discovery of dihydroisoquinolinone derivatives as novel inhibitors of the p53-MDM2 interaction with a distinct binding mode.

Gessier F, Kallen J, Jacoby E, Chène P, Stachyra-Valat T, Ruetz S, Jeay S, Holzer P, Masuya K, Furet P.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3621-5. doi: 10.1016/j.bmcl.2015.06.058. Epub 2015 Jun 23.

PMID:
26141769
18.

An ultrahigh affinity d-peptide antagonist Of MDM2.

Zhan C, Zhao L, Wei X, Wu X, Chen X, Yuan W, Lu WY, Pazgier M, Lu W.

J Med Chem. 2012 Jul 12;55(13):6237-41. doi: 10.1021/jm3005465. Epub 2012 Jun 22.

19.

Small-molecule inhibitors of the MDM2-p53 protein-protein interaction based on an isoindolinone scaffold.

Hardcastle IR, Ahmed SU, Atkins H, Farnie G, Golding BT, Griffin RJ, Guyenne S, Hutton C, Källblad P, Kemp SJ, Kitching MS, Newell DR, Norbedo S, Northen JS, Reid RJ, Saravanan K, Willems HM, Lunec J.

J Med Chem. 2006 Oct 19;49(21):6209-21.

PMID:
17034127
20.

Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.

Ding K, Lu Y, Nikolovska-Coleska Z, Wang G, Qiu S, Shangary S, Gao W, Qin D, Stuckey J, Krajewski K, Roller PP, Wang S.

J Med Chem. 2006 Jun 15;49(12):3432-5.

PMID:
16759082

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