Triarylethylene-indolin-2,3-dione molecular conjugates: design, synthesis, docking studies and anti-proliferation evaluation

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Triarylethylene-indolin-2,3-dione molecular conjugates: design, synthesis, docking studies and anti-proliferation evaluation

机译：三亚甲基 - 吲哚啉-2,3-二酮分子缀合物：设计，合成，对接研究和抗扩散评估

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A series of 1H-1,2,3-triazole-linked ospemifene-isatin and O-methylated ospemifene-isatin conjugates were synthesized and assayed for their anti-proliferative activities against estrogen-responsive as well as estrogen-non-responsive cells. The non-cytotoxic conjugate 14e, with an optimal combination of bromo substituents at the C-5/C-7 positions of isatin, proved to be a promising hit with an IC50 value of 31.62 mu M against MCF-7 and 19.23 mu M against MDA-MB-231. The observed anti-proliferative activities of active conjugates were further corroborated via docking studies carried out on estrogen receptor subtypes alpha and beta.

机译：合成了一系列1H-1,2,3-三唑型和O-甲基化OSPemifene-Isatin缀合物并测定其对雌激素响应性的抗增殖活动以及雌激素 - 非响应细胞。非细胞毒性缀合物14E，在Isatin的C-5 / C-7位置的溴代取代基的最佳组合证明是对MCF-7和19.23μm的IC50值为31.62 mu m的有希望的击球 MDA-MB-231。通过对雌激素受体亚型α和β进行的对接研究进一步证实了活性缀合物的观察到的活性缀合物的抗增殖活性。

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《RSC Advances》 |2019年第72期|共6页
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机译：三亚甲基 - 吲哚啉-2,3-二酮分子缀合物：设计，合成，对接研究和抗扩散评估
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Triarylethylene-indolin-2,3-dione molecular conjugates: design, synthesis, docking studies and anti-proliferation evaluation

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