SM-1, a novel PAC-1 derivative, activates procaspase-3 and causes cancer cell apoptosis

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• 作者：Yanfen Chen ; Meng Sun ; Jingsong Ding ; Qubo Zhu
• 关键词：SM ; 1 ; PAC ; 1 ; Caspase ; 3 ; Apoptosis ; Antitumor drug
• 刊名：Cancer Chemotherapy and Pharmacology
• 出版年：2016
• 出版时间：September 2016
• 年：2016
• 卷：78
• 期：3
• 页码：643-654
• 全文大小：7,940 KB
• 刊物类别：Biomedical and Life Sciences
• 刊物主题：Biomedicine
  Cancer Research
  Pharmacology and Toxicology
  Oncology
  
• 出版者：Springer Berlin / Heidelberg
• ISSN：1432-0843
• 卷排序：78

文摘

PurposeTo develop more potent procaspase-3 activator, 7 novel derivatives of PAC-1 were synthesized and evaluated. Among them, SM-1 stood out for its promising activity and good pharmacokinetics properties. The purpose of this study is to elucidate the pharmacological mechanism of SM-1 and evaluate its efficacy and toxicity in-depth.