Synthesis and cytotoxic evaluation of novel indenoisoquinoline-substituted triazole hybrids

详细信息    查看全文

• 作者：Tham Pham Thi^a ; ^b ; Thuy Giang Le Nhat^a ; Thuong Ngo Hanh^a ; Tan Luc Quang^a ; ^c ; Chinh Pham The^a ; ^d ; Tuyet Anh Dang Thi^a ; Ha Thanh Nguyen^a ; Thu Ha Nguyen^a ; Phuong Hoang Thi^a ; Tuyen Van Nguyen^a ; ^{ngvtuyen@hotmail.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Indenoisoquinolines ; Triazole ; AZT ; Hybrids ; Cytotoxic agents
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：1 August 2016
• 年：2016
• 卷：26
• 期：15
• 页码：3652-3657
• 全文大小：1346 K

文摘

The synthesis of various substituted triazole–indenoisoquinoline hybrids was performed based on a CuI-catalyzed 1,3-cycloaddition between propargyl-substituted derivatives and the azide-containing indenoisoquinoline. Besides, a variety of N-(alkyl)propargylindenoisoquinolines was used as substrates for the construction of triazole–indenoisoquinoline–AZT conjugated via a click chemistry-mediated coupling with 3′-azido-3′-deoxythymidine (AZT). Thus, twenty three new indenoisoquinoline-substituted triazole hybrids were successfully prepared and evaluated as cytotoxic agents, revealing an interesting anticancer activity of four triazole linker–indenoisoquinoline–AZT hybrids in KB and HepG2 cancer cell lines.