2. Academic Validation
  3. Synthesis and cytotoxic evaluation of novel indenoisoquinoline-substituted triazole hybrids

Synthesis and cytotoxic evaluation of novel indenoisoquinoline-substituted triazole hybrids

  • Bioorg Med Chem Lett. 2016 Aug 1;26(15):3652-7. doi: 10.1016/j.bmcl.2016.05.092.
Tham Pham Thi 1,  Thuy Giang Le Nhat 2,  Thuong Ngo Hanh 2,  Tan Luc Quang 3,  Chinh Pham The 4,  Tuyet Anh Dang Thi 2,  Ha Thanh Nguyen 2,  Thu Ha Nguyen 2,  Phuong Hoang Thi 2,  Tuyen Van Nguyen 5
Affiliations

Affiliations

  • 1 Institute of Chemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam; Thuyloi University, 175, Tay Son, Hanoi, Vietnam.
  • 2 Institute of Chemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam.
  • 3 Institute of Chemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam; Hanoi Pedagogical University No. 2, Vietnam.
  • 4 Institute of Chemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam; Thainguyen University of Science, Tanthinh, Thainguyen, Vietnam.
  • 5 Institute of Chemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam. Electronic address: ngvtuyen@hotmail.com.
PMID: 27342752 DOI: 10.1016/j.bmcl.2016.05.092
Abstract

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.

Keywords

AZT; Cytotoxic agents; Hybrids; Indenoisoquinolines; Triazole.

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