Departamento de Química, Universidade Federal de São Carlos - UFSCar, São Carlos, SP, Brazil.
Laboratório de Síntesis Orgánica, Facultad de Química, Universidad de La Habana - UH, Habana, Cuba.
Mater Sci Eng C Mater Biol Appl. 2020 Oct;115:111106. doi: 10.1016/j.msec.2020.111106. Epub 2020 May 20.
Five new complexes with general formula [Ru(L)(PP)(bipy)]PF, where L = N,N'-dimethyl-N-Acyl thiourea, and P-P: 1,2-bis(diphenylphosphino)ethane (dppe) or 1,4-bis(diphenylphosphino)butane (dppb)) were synthesized and characterized by elemental analysis, molar conductivity, cyclic voltammetry, IR, NMR (H, C{H} and P{H}), and single crystal X-ray diffractometry. The cytotoxicity of compounds against lung and breast tumor cell lines was significant, where two complexes, [Ru(L)(bipy)(dppe)]PF (3) and [Ru(L)(bipy)(dppb)]PF (6), were selected to evaluate changes in morphology, inhibition of migration and cell death in the MDA-MB-231 lineage. The complexes caused alterations in the cell morphology and were able to inhibit cell migration at the concentrations evaluated, induce the cell cycle arrested in the Sub-G1 phase, and induced cell death by apoptosis. All the complexes presented interaction with HSA, and the interaction studies with DNA suggested weak interactions, probably by the minor groove.
合成了五个新的配合物，其通式为[Ru(L)(PP)(bipy)]PF，其中 L = N,N'-二甲基-N-酰基硫脲，P-P 为 1,2-双（二苯基膦）乙烷（dppe）或 1,4-双（二苯基膦）丁烷（dppb）），并用元素分析、摩尔电导率、循环伏安法、IR、NMR（H、C{H} 和 P{H}）和单晶 X 射线衍射法进行了表征。这些化合物对肺癌和乳腺癌肿瘤细胞系的细胞毒性显著，其中两个配合物[Ru(L)(bipy)(dppe)]PF（3）和[Ru(L)(bipy)(dppb)]PF（6）被选择来评估 MDA-MB-231 系细胞形态的变化、迁移抑制和细胞死亡。这些配合物导致细胞形态发生变化，并能在评估的浓度下抑制细胞迁移，诱导细胞周期停滞在 Sub-G1 期，并通过细胞凋亡诱导细胞死亡。所有配合物均与 HSA 相互作用，与 DNA 的相互作用研究表明存在弱相互作用，可能通过小沟。
