Synthesis and biological evaluation of water-soluble <i>trans</i>-[bicyclo[2.2.2]octane-7<i>R</i>,8<i>R</i>-diamine]platinum(II) complexes with linear or branched alkoxyacetates as leaving groups
作者:Fengfan Liu、Weiwei Hu、Lei Fang、Shaohua Gou
DOI:10.1080/00958972.2016.1163546
日期:2016.4.2
Abstract Four platinum(II) complexes, trans-[bicyclo[2.2.2]octane-7R,8R-diamine]bis(alkoxyacetato-O,O’) platinum(II) (alkoxyacetate = methoxyacetate (2), ethoxyacetate (3), isopropoxyacetate (4), and tert-butoxyacetate (5)) were synthesized and spectrally characterized. The cytotoxicity of these water-soluble complexes was evaluated by CCK-8 assay in vitro against HCT-116, HepG-2, and A549 cancer cell
摘要 四种铂(II)配合物,反式-[双环[2.2.2]辛烷-7R,8R-二胺]双(烷氧基乙酸根-O,O')铂(II)(烷氧基乙酸盐=甲氧基乙酸盐(2),乙氧基乙酸盐(3) 、异丙氧基乙酸酯 (4) 和叔丁氧基乙酸酯 (5)) 被合成并进行光谱表征。这些水溶性复合物的细胞毒性通过 CCK-8 体外试验对 HCT-116、HepG-2 和 A549 癌细胞系进行评估。大多数复合物对测试的癌细胞系具有细胞毒活性。其中,3种显示出比顺铂或奥沙利铂更有效的抗肿瘤作用。复合物 3 可导致基于凋亡途径的 HCT-116 细胞系死亡,因为它具有类似于奥沙利铂中的 1R,2R-二氨基环己烷的双环部分。