Novel Derivatives Based on Zerumbone Scaffold as Potential Anticancer Inhibitors

Author:

Hung Truong Ngoc1,Chinh Luu Van1,Hieu Luu Xuan2,Ha Tran Thi Hong1,Chi Hoang Kim1,Vu Tran Khac3,Chung Pham Van4

Affiliation:

1. Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology (VAST), 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam

2. Technical Department of Vinhphuc Police, Vinh Yen, Vinh Phuc, Vietnam

3. School of Chemical Engineering, Hanoi University of Science and Technology, No.1, Dai Co Viet, Hai Ba Trung, Hanoi, Vietnam

4. Pharmaceutical Chemistry and Pharmaceutical Technology Application Joint Stock Company, 45/24 Dien Bien Phu, Ngo Quyen, Haiphong, Vietnam

Abstract

Abstract: A two-step procedure was applied to couple zerumbone, a natural sesquiterpene, with thiols 8a-k to obtain a small library of ten novel zerumbone derivatives 9a-k with full-length library data of spectra including 1H-, 13C-NMR, and HRMS. The tautomerization of 9a, 9b, and 9c was revealed in DMSO and discussed in the case of 9c. The series of 9a-k together with zerumbone 1 was evaluated for their in vitro cytotoxic activity using three human cancer cell lines, HepG2, A549 and HeLa. The results revealed that all zerumbone derivatives had cytotoxic activity against HepG2, A549, and HeLa cells that was 4-20 times stronger than zerumbone.

Publisher

Bentham Science Publishers Ltd.

Subject

Organic Chemistry,Biochemistry

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