Structure-activity relationships of new Organotin(IV) anticancer agents and their cytotoxicity profile on HL-60, MCF-7 and HeLa human cancer cell lines
作者:Hussain Ullah、Viola Previtali、Helene B. Mihigo、Brendan Twamley、Muhammad Khawar Rauf、Fatima Javed、Amir Waseem、Robert J. Baker、Isabel Rozas
DOI:10.1016/j.ejmech.2019.07.047
日期:2019.11
intercalation. Complexes having n-butyl substituents were more potent and cytotoxic against human leukemia, breast and cervical cancer cell lines than other organotin(IV) complexes tested. Unfortunately, some of these compounds showed similar cytotoxicity in a non-cancerous cell line. We may conclude that cytotoxic activity was dependent on the nature (lipophilicity and size, according to the structure-activity
人们越来越关注有机锡(IV)化合物对癌细胞生长的抑制作用,因此,一系列新的二甲基,二(正丁基),二苯基和氯苯基锡(IV)配合物与准备了希夫基核。通过不显示相互作用的UV热变性和通过插层显示适度相互作用的UV-vis滴定法评估它们与DNA的结合。具有正丁基取代基的配合物比其他测试的有机锡(IV)配合物对人白血病,乳腺癌和子宫颈癌细胞系更有效且具有细胞毒性。不幸的是,这些化合物中的一些在非癌细胞系中显示出相似的细胞毒性。我们可以得出结论,细胞毒性活性取决于自然(亲脂性和大小,根据结构-活性关系研究)和不同结构上的取代模式。这些结果可能有助于合理设计金属药物,扩大有机锡复合物的范围,从而配制具有二丁基部分的新型金属基药物。