Affiliation:
1. Department of Pharmacy, Hengyang Medicinal School, University of South China, Hunan Provincial Key Laboratory
of Tumor Microenvironment Responsive Drug Research, Hunan Province Cooperative Innovation Center for Molecular
Target New Drug Study, The Second Affiliated Hospital of University of South China, Hengyang, Hunan, 421001, China
Abstract
Background:
Genistein has been limited in clinical application due to its low bioavailability, extremely poor liposolubility, and fast glycosylation rate, though it possesses anti-breast cancer activity. Therefore, the discovery of novel genistein derivatives is an urgency.
Objective:
To enhance the anti-breast cancer activity of genistein, a series of novel fluorinated genistein derivatives were synthesized.
Method:
Their in vitro antitumor activity was investigated by the MTT assay against three cancer cell lines, via., MDA-MB-231, MCF-7 and MDA-MB-435, respectively.
Results:
Analogs 1d, 2b, 3b showed remarkable anticancer activities comparing to tamoxifen, a clinical anti-breast cancer drug on the market.
Conclusion:
The activities against breast cancer of genistein were enhanced by introducing 7-alkoxyl group and fluorine atom into the B-ring. Therefore, these compounds may be potential candidates for treating breast cancer.
Funder
Natural Science Foundation of Hunan
Hunan Provincial Hengyang Joint Fund
Laboratory of Tea and Health of Hengyang
Undergraduate Research Learning, and Innovative Experiment Project
Publisher
Bentham Science Publishers Ltd.
Cited by
3 articles.
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