Yang Zhifang, Liu Yi, Liu Zhuo, Xu Qinfang, Liu Shun, Jiang Kailin, Shi Yuanlong, Xu Wenyu, Yang Zehua, Mi Pengbing, Xiang Yijun, Yao Xu, Zheng Xing
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.
Med Chem. 2022;19(1):64-74. doi: 10.2174/1573406418666220607140651.
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.
To enhance the anti-breast cancer activity of genistein, a series of novel fluorinated genistein derivatives were synthesized.
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.
Analogs 1d, 2b, and 3b showed remarkable anticancer activities compared to tamoxifen, a clinical anti-breast cancer drug on the market.
The activities against breast cancer of genistein were enhanced by introducing the 7- alkoxyl group and fluorine atom into the B-ring. Therefore, these compounds may be potential candidates for treating breast cancer.
尽管染料木黄酮具有抗乳腺癌活性，但其生物利用度低、脂溶性极差且糖基化速率快，限制了其临床应用。因此，迫切需要发现新型染料木黄酮衍生物。
为增强染料木黄酮的抗乳腺癌活性，合成了一系列新型氟化染料木黄酮衍生物。
通过MTT法分别检测其对三种癌细胞系MDA-MB-231、MCF-7和MDA-MB-435的体外抗肿瘤活性。
与市场上的临床抗乳腺癌药物他莫昔芬相比，类似物1d、2b和3b表现出显著的抗癌活性。
通过在B环引入7-烷氧基和氟原子，增强了染料木黄酮对乳腺癌的活性。因此，这些化合物可能是治疗乳腺癌的潜在候选药物。
