Synthesis and anti-cancer activity of bis-amino-phosphine ligand and its ruthenium(II) complexes
作者:Zelinda Engelbrecht、Kim Elli Roberts、Ayesha Hussan、Gershon Amenuvor、Marianne Jaqueline Cronjé、James Darkwa、Banothile C.E. Makhubela、Lungile Sitole
DOI:10.1016/j.bmcl.2020.127492
日期:2020.10
determined for both the complexes, the ligand and cisplatin, for comparison. Both complexes GA105 and GA113 displayed a high anti-cancer selectivity profile as they exhibited low IC50 values of 6.72 µM and 8.76 µM respectively, with low toxicity towards a non-malignant human cell line. The IC50 values obtained for both complexes were lower than that of cisplatin. The new complexes were more effective compared
化疗药物耐药性和不良副作用的发展表明,当前的化疗药物在治疗各种类型的癌症方面仍然无效。因此,需要开发具有抗癌活性的新金属药物。钌配合物由于其有希望的抗肿瘤特性和降低的体内毒性而引起了人们的极大兴趣。这项研究强调了两种新型的双氨基膦钌(II)配合物GA105和GA113有效诱导恶性黑色素瘤细胞死亡。测定复合物,配体和顺铂的IC 50浓度,以进行比较。两种配合物GA105GA113和GA113分别具有低的IC 50值(6.72 µM和8.76 µM),并且对非恶性人类细胞系的毒性低,因此具有较高的抗癌选择性。两种复合物的IC 50值均低于顺铂。与游离配体GA103(IC 50 => 20 µM)相比,新的复合物更有效。对处理过的细胞的形态学研究诱导了凋亡特征,进一步的研究可能表明了内在的细胞死亡途径。此外,流式细胞仪分析显示,复杂GA113的细胞死亡方式是凋亡。本文的结果为将来进一步了解选定的