Affiliation:
1. School of Chemical Engineering, Hanoi University of Science and Technology, 1 Dại Co Viet, Bach Khoa, Hai Ba Trung, Ha Noi, Vietnam
Abstract
Background:
A series of new zerumbone hydrazones 5a-f and 9a-f have been synthesized
in via an in situ procedure in high yields. The structure of synthesized compounds has been
confirmed using 1H, 13C NMR and HR-MS. The bioassay result showed that several compounds exhibited
cytotoxic effects against three human cancer cell lines, including HepG-2, SK-LU-1, and
MCF-7. Compound 9a showed the best cytotoxic effect against HepG-2, SK-LU-1, and MCF-7
with IC50 values of 8.20, 6.66, and 9.35 μM, respectively.
Objective:
This study aims at developing new zerumbone hydrazones as anticancer agents based
on zerumbone, a natural compound wildly growing in Vietnam.
Methods:
A series of new zerumbone hydrazones was designed, synthesized, and evaluated for cytotoxicity
against three human cancer cell lines, including HepG-2, MCF-7, and SKLu-1, using the
MTT method.
Results:
The bioassay result showed that several compounds exhibited cytotoxic effects against
three human cancer cell lines, including HepG-2, SK-LU-1, and MCF-7. Especially, compound 9a
displayed the best cytotoxic effect against HepG-2, SK-LU-1, and MCF-7 with IC50 values of 8.20,
6.66, and 9.35 μM, respectively.
Conclusion:
The research results suggest that some compounds could be considered as leads for
the future design of zerumbone hydrazones in which bio-isosteric replacements in theortho position
of the phenyl ring could be performed to improve the cytotoxic activity.
Funder
National Fundation for Science and Technology of Vietnam
Publisher
Bentham Science Publishers Ltd.
Subject
General Pharmacology, Toxicology and Pharmaceutics
Cited by
3 articles.
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