Terminal functionalized thiourea-containing dipeptides as multidrug-resistance reversers that target 20S proteasome and cell proliferation

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• 作者：Jian-Mei Qin^a ; ¹ ; Ri-Zhen Huang^b ; ¹ ; Gui-Yang Yao^b ; Zhi-Xin Liao^b ; Ying-Ming Pan^a ; ^{panym2013@hotmail.com} ; Heng-Shan Wang^a ; ^{whengshan@163.com}
• 关键词：Pseudopeptides ; Thioureas ; Proteasome ; Anti-tumor ; Multidrug resistance
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：259-269
• 全文大小：1757 K
• 卷排序：126

文摘

A novel series of the terminal functionalized dipeptides derivatives containing thiourea group moiety were synthesized. Compound 6i exhibited remarkable ChT-L proteasome inhibitory activity. Molecular modeling suggested that 6i tightly binds to the active site of 20S proteasome. The inhibitors efficiently block survival of doxorubicin-resistant human lung cancer cells. 6i induced apoptosis in NCI-H460 and NCI-H460/DOX cells.