Synthesis of novel curcumin mimics and preliminary evaluation for their antitumor activity.
- Author:
Yong-Cheng WANG
;
Yu-Shan LI
;
Han-Ze YANG
;
Yan LI
;
Xiao-Guang CHEN
;
Zhi-Qiang FENG
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
pharmacology;
Cell Line, Tumor;
Curcumin;
analogs & derivatives;
chemical synthesis;
pharmacology;
Drug Screening Assays, Antitumor;
Humans;
Inhibitory Concentration 50
- From:
Acta Pharmaceutica Sinica
2014;49(7):1022-1028
- CountryChina
- Language:Chinese
-
Abstract:
Curcumin has been reported to possess antitumor activity with low toxicity. However, the clinical application of curcumin has been significantly limited by its instability and poor metabolic property. In order to overcome these limitations and discover novel small molecules with potential antitumor activity, 29 curcumin mimics were synthesized, which were confirmed by 1H NMR and HR-MS, and their cytotoxic property was evaluated against five human cancer cell lines in vitro. Compounds 16, 18 and 19 exhibited good cytotoxic property, their IC50 value were even below 5 micromol x L(-1) to some cancer cell lines, 5-9 times better than curcumin.
