Design, Synthesis and Biological Evaluation of Sulfamide and Triazole Benzodiazepines as Novel p53-MDM2 Inhibitors

Design, Synthesis and Biological Evaluation of Sulfamide and Triazole Benzodiazepines as Novel p53-MDM2 Inhibitors

A series of sulfamide and triazole benzodiazepines were obtained with the principle of bioisosterism. The p53-murine double minute 2 (MDM2) inhibitory activity and in vitro antitumor activity were evaluated. Most of the novel benzodiazepines exhibited moderate protein binding inhibitory activity. Pa...

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Bibliographic Details
Main Authors: Zhiliang Yu, Chunlin Zhuang, Yuelin Wu, Zizhao Guo, Jin Li, Guoqiang Dong, Jianzhong Yao, Chunquan Sheng, Zhenyuan Miao, Wannian Zhang
Format: Article
Language:English
Published: MDPI AG 2014-09-01
Series:International Journal of Molecular Sciences
Subjects:
p53-MDM2
small molecule inhibitors
sulfamidebenzodiazepine
triazolebenzodiazepine
antitumor activity
Online Access:http://www.mdpi.com/1422-0067/15/9/15741

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http://www.mdpi.com/1422-0067/15/9/15741

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