Design and synthesis of novel tetrandrine derivatives as potential anti-tumor agents against human hepatocellular carcinoma

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• 作者：Junjie Lan^a ; ^c ; ^d ; ¹ ; Ning Wang^b ; ¹ ; Lan Huang^a ; ^c ; Yazhou Liu^a ; ^c ; Xiaopan Ma^a ; ^c ; Huayong Lou^a ; ^c ; Chao Chen^a ; ^c ; Yibin Feng^b ; ^yfeng@hku.hk ; Weidong Pan^a ; ^c ; ^{wdpan@163.com}
• 关键词：Tetrandrine ; Hepatocellular carcinoma ; Apoptosis ; ER stress ; JNK
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：554-566
• 全文大小：1833 K
• 卷排序：127

文摘

35 Amide substituted tetrandrine derivatives were designed and synthesized. Most derivatives showed good anti HCC activity and compound 31 showed the strongest activity. Amide was the key pharmacophore for anti-cancer activity. Inducement of apoptosis of HCC cells might be the mechanisms of action of compound 31. Compound 31 could also initiate endoplasmic reticulum stress and activate JNK.