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Design, Synthesis, and Anti-Breast Cancer Activity of Novel Fluorinated 7-O-Modified Genistein Derivatives

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成果类型:
期刊论文
作者:
Yang, Zhifang;Liu, Yi;Liu, Zhuo;Xu, Qinfang;Liu, Shun;...
作者机构:
[Xiang, Yijun; Xu, Qinfang; Shi, Yuanlong; Yang, Zhifang; Zheng, Xing; Yang, Zehua; Mi, Pengbing; Liu, Yi; Jiang, Kailin; Yao, Xu; Liu, Zhuo; Xu, Wenyu; Liu, Shun] Univ South China, Affiliated Hosp 2, Hunan Prov Cooperat Innovat Ctr Mol Target New Dru, Hengyang Med Sch,Dept Pharm,Hunan Prov Key Lab Tum, Hengyang 421001, Hunan, Peoples R China.
语种:
英文
关键词:
Anti-breast cancer activities;Baker-Venkataraman reaction;Fluorinated-genistein derivatives;Genistein;MTT assay;structure-activity relationship
期刊:
MEDICINAL CHEMISTRY
ISSN:
1573-4064
年:
2023
卷:
19
期:
1
页码:
64-74
基金类别:
Natural Science Foundation of Hunan [2021JJ80015]; Hunan Provincial Hengyang Joint Fund [2020JJ6052]; Undergraduate Research Learning and Innovative Experiment Project [X202110555454, X202110555467, X202110555473, 202150083704]; Laboratory of Tea and Health of Hengyang; [S202010555176]
机构署名:
本校为第一机构
院系归属:
药学与生物科学学院
摘要:
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.Methods: 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, a...

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