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Letters in Organic Chemistry

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ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

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Research Article

Design, Synthesis and In vitro Cytotoxic Evaluation of Novel Hybrids of Artemisinin and Quinazolinone

Author(s): Tran Khac Vu*, Bach Xuan Nguyen, Linh Nguyen Pham Duy, Thuc Bao Nguyen Truong, Anh Tuan Phung, Nguyen Thi Bich Phuong, Tran Thi Hai Van and Thi Xuan Vu

Volume 19, Issue 7, 2022

Published on: 13 January, 2022

Page: [558 - 569] Pages: 12

DOI: 10.2174/1570178618666211001115131

Price: $65

Abstract

In this study, two novel hybrid series of artemisinin and quinazolinones were synthesized and evaluated in vitro cytotoxicity against two human cancer cell lines, including SKLu-1 (lung cancer), MCF- 7 (breast cancer). The bio-assay results indicated that most of the target compounds exhibited cytotoxic activities against both human cancer cell lines tested and seemed to be more cytotoxic toward the breast (MCF-7) cancer cells than lung (SKLu-1) cancer cells. Among the synthesized artemisinin hybrids, the compound 13d containing a quinazolinone conjugated system exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 μM, respectively. This study aims at developing novel hybrids of artemisinin and quinazolinones as anti-cancer agents. A series of novel hybrids were designed, synthesized, and evaluated for cytotoxicity against two human cancer cell lines, including SKLu- 1 and MCF-7, using the SRB method. All thirteen hybrids of artemisinin with quinazolinone exhibited cytotoxic activity against two tested cancer cell lines, in which the compound 13d exhibited the most potent cytotoxicity against the SKLu-1 and MCF-7 cell lines with IC50 values of 1.62 and 0.77 μM, respectively. The research results suggest that some compounds could be considered as leads for future design of hybrids and have the potential for further studies in the field of anti-cancer agent development.

Keywords: Anti-cancer, artemisinin, cell line, cytotoxicity, dihydroartemisinin, hybrid, quinazolinone.

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