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Drug Dev Res. 2016 Feb;77(1):43-9. doi: 10.1002/ddr.21291. Epub 2016 Feb 5.

Synthesis and Cytotoxic Evaluation of Monocarbonyl Analogs of Curcumin as Potential Anti-Tumor Agents.

Author information

1
The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu, People's Republic of China.
2
Department of Orthopedic Surgery, The First Affiliated Hospital, Wenzhou Medical University, Wenzhou, Zhejiang, People's Republic of China.

Abstract

Preclinical Research A series of mono-carbonyl curcumin analogs with different substituents at the 4/4'-position of the phenyl group were synthesized and screened for in vitro cytotoxicity against a panel of human cancer cell lines using a methyl thiazolyl tetrazolium assay. Several of the curcumin analogs, especially B114, exhibited a wide-spectrum of anti-tumor properties in all tested cell lines, indicating their potential in as anti-cancer lead compounds. Further toxicity testing in the NRK-52E kidney cell line revealed that the analogs A111, A113, and B114 had comparable or higher safety than curcumin. These data suggested that the introduction of appropriate substituents in the 4/4'-positions could be a promising approach for curcumin-based drug design.

KEYWORDS:

anti-tumor activity; monocarbonyl curcumin analogs; synthesis

PMID:
26846154
PMCID:
PMC4832843
DOI:
10.1002/ddr.21291
[Indexed for MEDLINE]
Free PMC Article

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