1. Synthesis of New Zerumbone Hydrazones and Their In-vitro Anticancer Activity
- Author
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Jadhav Ghanshyam, Ulaganathan Venkatasubramanian, Van Vu Vu, Moghaddam Vahed Mohammad, Wang Tian-Hao, L. Kaviarasan, Sivasubramanian Aravind, Sarkar Esha, Senthil Kumar Ramachandran, Medhane Vijay, A.A.M. Shalan Nor, Yi Feng, Deshmukh Dattatray, Lakshmana Rao A., Venkateswara Rao P., Rao Rekha, Jakhar Seema, A. Rahim Norhazira, Prasad S.V.U.M., Rajendran Narendran, Nainar Meyyanathan Subramania, Toorchi Mahmoud, Misra Aparna, Trivedi Anchal, Luo Ding, Monirifar Hassan, I. Mohamad Nur, Kalirajan Rajagopal, Tong Jian-Bo, Subramanian Shankar, Hosseini Maryam, Kadian Varsha, Makala Himesh, Khac Vu Tran, K. Balapure Anil, and Gowramma Bryan
- Subjects
Biochemistry ,Chemistry ,General Pharmacology, Toxicology and Pharmaceutics ,In vitro - 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.
- Published
- 2021