设计和合成二茂铁基 1,4-二氢吡啶及其作为驱动蛋白-5 抑制剂的评价。
Design and synthesis of ferrocenyl 1,4-dihydropyridines and their evaluation as kinesin-5 inhibitors.
机构信息
Laboratory of Molecular Spectroscopy, Department of Organic Chemistry, Faculty of Chemistry, University of Lodz, ul. Tamka 12, 91-403 Łódź, Poland.
Cytometry Lab, Department of Oncobiology and Epigenetics, Faculty of Biology and Environmental Protection, University of Lodz, ul. Pomorska 141/143, 90-236 Łódź, Poland.
出版信息
Dalton Trans. 2024 Oct 1;53(38):16038-16053. doi: 10.1039/d4dt01853b.
Kinesin-5 inhibitors offer cancer cell-targeted approach, thus securing reduced systemic toxicity compared to other antimitotic agents. By modifying the 1,4-dihydropyridine-based kinesin-5 inhibitor CPUYL064 with a ferrocenyl moiety (Fc), we designed and prepared a series of organometallic hybrids that show high antiproliferative activity, with the best compounds exhibiting up to 19-fold increased activity. This enhanced activity can be attributed to the presence of the ferrocenyl moiety.
驱动蛋白-5 抑制剂提供了一种针对癌细胞的方法，因此与其他抗有丝分裂剂相比，系统毒性降低。通过用二茂铁基部分（Fc）修饰基于 1,4-二氢吡啶的驱动蛋白-5 抑制剂 CPUYL064，我们设计并制备了一系列显示出高抗增殖活性的金属有机杂化物，其中最好的化合物的活性增加了 19 倍。这种增强的活性可以归因于二茂铁基部分的存在。
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