Chiang Mai Journal of Science

Synthesis of New Zerumbone Derivatives and Their In vitro Anti-cancer Activity

Paper Type	Contributed Paper
Title	Synthesis of New Zerumbone Derivatives and Their In vitro Anti-cancer Activity
Author	Vu Tien Chinh, Pham Thanh Loan, Vu Xuan Duong, Tran Khac Vu and Luu Van Chinh
Email	Chinhluuvan@gmail.com, vu.trankhac@hust.edu.vn
Abstract: Twelve novel derivatives (16-18, 21-23, 26, 27 and 31-34) of azazerumbone and azazerumbone oxide with dihydroartemisinin (DHA), zidovudine (AZT), [4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsunfonylamino) pyrimidin-5-yl] methanol (PM), benzotriazole and piperazine derivatives were synthesized by N-alkylation, acylation and click triazole cyclisation. Their structures were confirmed by 1D-, 2D-NMR and HRMS spectra. Screening for cytotoxicity indicated that the conjugates 21-23 of azazerumbone and azazerumbone oxide with DHA showed potent cytotoxic activity to human cancer cell lines including HepG-2, LU-1, RD and FL. In addition, the anti-mutagenic activity role of azazerumbone (4, 5) in the improvemrnt of cytotoxicity was also discussed.
Start & End Page	181 - 194
Received Date	2019-04-05
Revised Date
Accepted Date	2019-08-03
Full Text	Download
Keyword	azazerumbone, azazerumbone oxide, click reaction, N-alkylation and cytotoxicity
Volume	Vol.47 No.1 (January 2020)
DOI
Citation	Chinh V.T., Loan P.T., Duong V.X., Vu T.K. and Chinh L.V., Synthesis of New Zerumbone Derivatives and Their In vitro Anti-cancer Activity, Chiang Mai J. Sci., 2020; 47(1): 181-194.
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