Synthesis and Antitumor Activity of New Tetrahydrocurcumin Derivatives Via Click Reaction

Duan, Meitao and Mahal, Ahmed and Mohammed, Ban and Zhu, Yongyan and Tao, Huaming and Mai, Shaoyu and Al-Haideri, Maysoon and Zhu, Quanhong (2021) Synthesis and Antitumor Activity of New Tetrahydrocurcumin Derivatives Via Click Reaction. Natural Product Research, 36 (20). pp. 5268-5276. ISSN 1478-6419

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Abstract

Three new derivatives of tetrahydrocurcumin 6, 7 and 9 have been prepared as potent antitumor agents using copper(II)-catalyzed ‘click chemistry’. Their structures were identified using 1H-NMR, 13C-NMR and HRMS techniques. MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay has been carried out to investigate the in vitro cytotoxicity against human cervical carcinoma (HeLa), human lung adenocarcinoma (A549), human hepatoma carcinoma (HepG2) and human colon carcinoma (HCT-116). Compound 6 has showed significant inhibitory activity against HCT-116 cell line with an IC50 value of 17.86 μM compared to tetrahydrocurcumin (50.96 μM) and positive control etoposide (19.48 μM) while showed no inhibitory activity against NCM460 cell line. Compounds 7 showed moderate inhibitory activity compared to tetrahydrocurcumin and etoposide while compound 9 showed no obvious inhibitory activity. The results suggested further structure modifications of tetrahydrocurcumin to improve its anticancer activity.

Item Type: Article
Uncontrolled Keywords: Tetrahydrocurcumin ,Podophyllotoxin ,Click Reaction ,Antitumor Activity ,Drug Discovery
Subjects: Q Science > Q Science (General)
Divisions: Department of Medical Biochemical Analysis > Research papers
Depositing User: ePrints Depositor
Date Deposited: 06 Oct 2024 13:28
Last Modified: 06 Oct 2024 13:28
URI: https://eprints.cihanuniversity.edu.iq/id/eprint/1507

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