Difluoromethoxyestradiene-based steroid sulfatase (STS) inhibitors have been designed. Six difluoromethoxy-substituted steroid dervatives were synthesised and evaluated in vitro against the proliferation of MCF-7 and MDA MB-231 breast cancer cells. Bis-sulfamate 10 was identified as a promising antiproliferative agent (GI₅₀ 0.28 μM in MCF-7 cells), a potent STS inhibitor (IC₅₀ 3.7 nM in JEG-3 cells) and an inhibitor of tubulin assembly in vitro and colchicine binding to tubulin.

中文翻译：

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2-二氟甲氧基取代的雌三烯氨基磺酸酯：合成、抗增殖 SAR、抗微管蛋白活性和类固醇硫酸酯酶抑制

已经设计了基于二氟甲氧基雌二烯的类固醇硫酸酯酶 (STS) 抑制剂。合成了六种二氟甲氧基取代的类固醇衍生物，并在体外评估了它们对 MCF-7 和 MDA MB-231 乳腺癌细胞增殖的作用。双氨基磺酸10被确定为一种有前途的抗增殖剂（MCF-7 细胞中的 GI ₅₀ 0.28 μM）、一种有效的 STS 抑制剂（JEG-3 细胞中的 IC ₅₀ 3.7 nM）和体外微管蛋白组装抑制剂以及秋水仙碱与微管蛋白。