Synthesis and antitumor activity of new tetrahydrocurcumin derivatives via click reaction

Autor:	Ban Mohammed, Meitao Duan, Shaoyu Mai, Yongyan Zhu, Quanhong Zhu, Ahmed Mahal, Maysoon Al-Haideri, Huaming Tao
Rok vydání:	2021
Předmět:	biology Organic Chemistry Plant Science Pharmacology medicine.disease biology.organism_classification Biochemistry Analytical Chemistry HeLa chemistry.chemical_compound Podophyllotoxin chemistry Bromide Cell culture medicine Click chemistry Adenocarcinoma IC50 Etoposide medicine.drug
Zdroj:	Natural Product Research. 36:5268-5276
ISSN:	1478-6427 1478-6419
DOI:	10.1080/14786419.2021.1931181
Popis:	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.
Databáze:	OpenAIRE
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