Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development
Тип публикации: Journal Article
Дата публикации: 2014-02-05
SCImago Q1
Tоп 10% SCImago
WOS Q1
БС1
SJR: 1.726
CiteScore: 11.5
Impact factor: 6.8
ISSN: 00222623, 15204804
PubMed ID:
24456472
Drug Discovery
Molecular Medicine
Краткое описание
We recently reported the discovery of AM-8553 (1), a potent and selective piperidinone inhibitor of the MDM2-p53 interaction. Continued research investigation of the N-alkyl substituent of this series, focused in particular on a previously underutilized interaction in a shallow cleft on the MDM2 surface, led to the discovery of a one-carbon tethered sulfone which gave rise to substantial improvements in biochemical and cellular potency. Further investigation produced AMG 232 (2), which is currently being evaluated in human clinical trials for the treatment of cancer. Compound 2 is an extremely potent MDM2 inhibitor (SPR KD = 0.045 nM, SJSA-1 EdU IC50 = 9.1 nM), with remarkable pharmacokinetic properties and in vivo antitumor activity in the SJSA-1 osteosarcoma xenograft model (ED50 = 9.1 mg/kg).
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Sun D. et al. Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development // Journal of Medicinal Chemistry. 2014. Vol. 57. No. 4. pp. 1454-1472.
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Sun D. et al. Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development // Journal of Medicinal Chemistry. 2014. Vol. 57. No. 4. pp. 1454-1472.
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@article{2014_Sun,
author = {Daqing Sun and Zhihong Li and Yosup Rew and Michael Gribble and Michael D. Bartberger and Hilary P Beck and Jude Canon and Ada Chen and Xiaoqi Chen and David H. Chow and Jeffrey Deignan and Jason Duquette and John Eksterowicz and Benjamin Fisher and Brian M Fox and Jiasheng Fu and Ana Z Gonzalez and Felix González-López de Turiso and Jonathan B Houze and David Huang and Min Jiang and LIXIA JIN and Frank Kayser and Jiwen (jim) Liu and Mei-Chu Lo and Alexander M. Long and Brian Lucas and Lawrence R. McGee and Joel Mcintosh and Jeff Mihalic and Jonathan D. Oliner and Tao Osgood and Matthew L Peterson and Phillip M Roveto and Anne Y. Saiki and Paul Shaffer and Maria Toteva and Yingcai Wang and Yu Chung Wang and Sarah Wortman and Peter Yakowec and Xuelei Yan and Qiuping Ye and Dongyin Yu and Yu Ming and XIAONING ZHAO and Jing Zhou and Jiang Zhu and Steven H Olson and Julio C. Medina and others},
title = {Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development},
journal = {Journal of Medicinal Chemistry},
year = {2014},
volume = {57},
publisher = {American Chemical Society (ACS)},
month = {feb},
url = {https://doi.org/10.1021/jm401753e},
number = {4},
pages = {1454--1472},
doi = {10.1021/jm401753e}
}
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MLA
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Sun, Daqing, et al. “Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development.” Journal of Medicinal Chemistry, vol. 57, no. 4, Feb. 2014, pp. 1454-1472. https://doi.org/10.1021/jm401753e.
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