In:
Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 19, No. 1 ( 2023-01), p. 64-74
Abstract:
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.
Type of Medium:
Online Resource
ISSN:
1573-4064
DOI:
10.2174/1573406418666220607140651
Language:
English
Publisher:
Bentham Science Publishers Ltd.
Publication Date:
2023
SSG:
15,3