SYNTHESIS AND ANTICANCER ACTIVITY OF 11-AZAARTEMISININ DERIVATIVES BEARING 1,2,3-TRIAZOLE MOIETY

Authors

  • Dung Tien Nguyen Vietnam University of Traditional Medicine, 2 Tran Phu St., Ha Dong, Hanoi 100000, Vietnam
  • Thuong Hanh Ngo Vietnam University of Traditional Medicine, 2 Tran Phu St., Ha Dong, Hanoi 100000, Vietnam
  • Hien Thu Tran Hanoi University of Pharmacy, 15 Le Thanh Tong St., Hoan Kiem, Hanoi 100000, Vietnam
  • Thao Phuong Dinh Vietnam University of Traditional Medicine, 2 Tran Phu St., Ha Dong, Hanoi 100000, Vietnam
  • Phuong Thi Do Vietnam University of Traditional Medicine, 2 Tran Phu St., Ha Dong, Hanoi 100000, Vietnam
  • Hau Ba Nguyen Vietnam University of Traditional Medicine, 2 Tran Phu St., Ha Dong, Hanoi 100000, Vietnam
  • Linh Thi Phuong Tran Vietnam University of Traditional Medicine, 2 Tran Phu St., Ha Dong, Hanoi 100000, Vietnam
  • Hanh My Ta Vietnam University of Traditional Medicine, 2 Tran Phu St., Ha Dong, Hanoi 100000, Vietnam

DOI:

https://doi.org/10.1007/6242

Keywords:

artemisinin, azaartemisinin, 1, 2, 3-triazole, anticancer activity, click reaction.

Abstract

A series of new compounds were prepared under mild reaction conditions using click reaction of 11-azaartemisinin and various azides. All the synthesized compounds were fully characterized by spectral data and evaluated for their cytotoxic activity against KB and HepG2 cell lines. All synthesized artemisinin derivatives are more active than 11-azaartemisinin. Thirteen of the synthesized compounds displayed good cytotoxic activity against two human cancer cell lines, KB and HepG2, with half maximal inhibitory concentration values in a range of 4.27–70.40 μM. The most active derivative was the best to both KB and HepG2 cell lines with IC50 value of 10.18 and 4.27 μM, respectively.

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Published

2021-10-21

Issue

Vol. 57 No. 10 (2021)

Section

Original Papers