Truong, Ngoc Hung and Le, Duc Anh and Vu, Thi Ha and Cam, Thi Inh and Do, Huu Nghi and Nguyen, Manh Cuong and Tran, Khac Vu and Tran, Hanh Nguyen and Pham, Van Chung and Luu, Van Chinh (2025) Functionalization of Natural Compounds to Enhance the Bioactivity of Zerumbone in Cancer Chemotherapy. In: Recent Developments in Chemistry and Biochemistry Research Vol. 10. BP International, pp. 71-102. ISBN 978-93-48859-47-1
Full text not available from this repository.Abstract
The alkylation reaction was employed to conjugate zerumbone with 3-substituted quinazolinone-4(3H)-ones and quinolines, resulting in the synthesis of 11 novel conjugates. These conjugates were thoroughly characterized using 1D-, 2D-NMR, and HRMS spectral data. Their enhanced bioactivity was evaluated through anti-inflammatory assays, specifically by inhibiting NO production in RAW 267.4 cells. Additionally, their cytotoxic activity was assessed against three human cancer cell lines: HepG2, SK-LU-1, and MCF-7. The results demonstrated that all 11 conjugates exhibited significantly potent cytotoxic activity, with IC50 values ranging from 1.01 to 9.86 µg/mL, surpassing the efficacy of the parent compound zerumbone. Furthermore, in silico studies, including EGFR inhibitory activity through docking and molecular dynamics simulations, were conducted to identify the most potent compounds. These studies highlighted the key interactions of zerumbone derivatives 16a-k with critical amino acids in the active site of the EGFR (PDB ID 4HJO) protein.
Item Type: | Book Section |
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Subjects: | Souths Book > Biological Science |
Depositing User: | Unnamed user with email support@southsbook.com |
Date Deposited: | 17 Jan 2025 13:42 |
Last Modified: | 10 Apr 2025 12:31 |
URI: | http://openaccess.journals4promo.com/id/eprint/1689 |