Synthesis and cytotoxic evaluation of novel indenoisoquinoline-substituted triazole hybrids

被引:11
作者
Tham Pham Thi [1 ,2 ]
Thuy Giang Le Nhat [1 ]
Thuong Ngo Hanh [1 ]
Tan Luc Quang [1 ,3 ]
Chinh Pham The [1 ,4 ]
Tuyet Anh Dang Thi [1 ]
Ha Thanh Nguyen [1 ]
Thu Ha Nguyen [1 ]
Phuong Hoang Thi [1 ]
Tuyen Van Nguyen [1 ]
机构
[1] Vietnam Acad Sci & Technol, Inst Chem, 18 Hoang Quoc Viet, Hanoi, Vietnam
[2] Thuyloi Univ, 175 Tay Son, Hanoi, Vietnam
[3] Hanoi Pedag Univ 2, Phuc Yen Town, Vinh Phuc Provi, Vietnam
[4] Thainguyen Univ Sci, Tanthinh, Thainguyen, Vietnam
关键词
Indenoisoquinolines; Triazole; AZT; Hybrids; Cytotoxic agents; TOPOISOMERASE-I INHIBITORS; PANCREATIC-CANCER CELLS; MYELOID-LEUKEMIA CELLS; BIOLOGICAL EVALUATION; ANTICANCER AGENTS; ANTIPROLIFERATIVE ACTIVITY; CLICK CHEMISTRY; NITRATED INDENOISOQUINOLINES; DERIVATIVES SYNTHESIS; SELECTIVE INHIBITORS;
D O I
10.1016/j.bmcl.2016.05.092
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 2016 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3652 / 3657
页数:6
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