Novel dihydroartemisinin derivatives exhibiting anticancer and antimalarial activities

Le Duc Anh; Truong Ngoc Hung; Ninh Duc Ha; Cam Thi Inh; Nguyen Trong Dan; Nguyen Van Thinh; Le Quang Tien; Cao Quoc Anh; Luu Van Chinh

doi:10.15625/2525-2518/20293

Author affiliations

Authors

Le Duc Anh \(^1\) Institute of Materials, Biology and Environment, Academy of Military Science and Technology, 17 Hoang Sam street, Nghia Do ward, Ha Noi, Viet Nam https://orcid.org/0000-0003-4954-620X
Truong Ngoc Hung \(^2\) Institute of Chemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet street, Nghia Do ward, Ha Noi, Viet Nam
Ninh Duc Ha \(^1\) Institute of Materials, Biology and Environment, Academy of Military Science and Technology, 17 Hoang Sam street, Nghia Do ward, Ha Noi, Viet Nam
Cam Thi Inh \(^2\) Institute of Chemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet street, Nghia Do ward, Ha Noi, Viet Nam
Nguyen Trong Dan \(^3\) Joint Vietnam - Russia Tropical Science and Technology Research Center, 63 Nguyen Van Huyen street, Nghia Do ward, Ha Noi, Viet Nam
Nguyen Van Thinh \(^3\) Joint Vietnam - Russia Tropical Science and Technology Research Center, 63 Nguyen Van Huyen street, Nghia Do ward, Ha Noi, Viet Nam
Le Quang Tien \(^4\) Faculty of Chemistry, VNU University of Science, Vietnam National University, 19 Le Thanh Tong street, Cua Nam ward, Ha Noi, Viet Nam
Cao Quoc Anh \(^4\) Faculty of Chemistry, VNU University of Science, Vietnam National University, 19 Le Thanh Tong street, Cua Nam ward, Ha Noi, Viet Nam
Luu Van Chinh \(^2\) Institute of Chemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet street, Nghia Do ward, Ha Noi, Viet Nam https://orcid.org/0000-0002-9476-0734

DOI:

https://doi.org/10.15625/2525-2518/20293

Keywords:

artemisinin, dihydroartemisinin, antimalarial, cytotoxicity

Abstract

A two-step procedure was used for the synthesis of six novel derivatives of artemisinin, a main active sesquiterpene lactone, which could be easily isolated on a large scale from the traditional medicinal plant Artemisia annua L in Vietnam. Structures of the prepared derivatives were characterized by full-length data of spectra, including ¹H-, ¹³C-NMR and HRMS. Screening for their in vitro cytotoxic activity was performed together with dihydroartemisinin (DHA) against three human cancer cell lines: HepG2, A549, and HeLa. Additionally, these derivatives were evaluated for antimalarial activity against P. plasmodium using the chloroquine-resistant strain (K1) and the chloroquine-sensitive strain (T96). The results showed that the prepared derivatives exhibited the cytotoxic activity against HepG2, LU-1, and HeLa cells with IC₅₀ values ranging from 1.32-18.38 µg/mL, which were stronger than that of DHA. Moreover, the anti-malarial results were promising for the development of new anti-malarial drugs.

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