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
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