Zhifang Yang 1 , Yi Liu 1 , Zhuo Liu 1 , Qinfang Xu 1 , Shun Liu 1 , Kailin Jiang 1 , Yuanlong Shi 1 , Wenyu Xu 1 , Zehua Yang 1 , Pengbing Mi 1 , Yijun Xiang 1 , Xu Yao 1 , Xing Zheng 1 Show Affiliations »
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.
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. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.
Entities: Chemical
Keywords:
Anti-breast cancer activities; Baker-Venkataraman reaction; Fluorinated-genistein derivatives; Genistein; MTT assay; structure-activity relationship
Year: 2022
PMID： 35674304 DOI： 10.2174/1573406418666220607140651
Source DB: PubMed Journal: Med Chem ISSN： 1573-4064 Impact factor: 2.745