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Azide-alkyne cycloaddition en route to ferrocenyl-methoxy-methyl-isatin-conjugates: Synthesis, anti-breast cancer activities and molecular docking studies
Journal of Organometallic Chemistry ( IF 2.3 ) Pub Date : 2019-12-10 , DOI: 10.1016/j.jorganchem.2019.121072
Anu Rani , Gurjot Inder Singh , Ramandeep Kaur , Gabriella Palma , Shanen Perumal , Mandeep Kaur , Oluwakemi Ebenezer , Paul Awolade , Parvesh Singh , Vipan Kumar

A series of 1H-1,2,3-triazole linked Ferrocenyl-methoxy-methyl-Isatin conjugates was synthesized and assayed for their anti-proliferative activities against estrogen-responsive as well as estrogen non-responsive cell lines. The non-cytotoxic conjugate 7l, with an optimum combination of octyl chain as spacer and methyl-substituent at the C-5 position of isatin, proved to be a promising hit with an IC50 value of 14.62 μM against MCF-7 and 79.63 μM against MDA-MB-231 cells, respectively. The observed anti-proliferative activities of active conjugates were further corroborated via docking studies carried out on estrogen receptor subtypes α and β.



中文翻译:

叠氮化物-炔环加成途中到二茂铁基甲氧基甲基靛红-缀合物的合成,抗乳腺癌活动和分子对接研究

合成了一系列的1 H -1,2,3-三唑连接的二茂铁基-甲氧基-甲基-靛红共轭物,并测定了它们对雌激素反应性和非雌激素反应性细胞系的抗增殖活性。非细胞毒性缀合物7l具有最佳的辛基链间隔基和在isatin的C-5位置的甲基取代基的最佳组合,被证明是很有前途的产品,相对于MCF-7和IC.79 ,IC 50值分别为14.62μM和79.63μM分别针对MDA-MB-231细胞。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所观察到的活性缀合物的抗增殖活性。

更新日期:2019-12-11
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