This work describes the synthesis, characterization and biological evaluation of three platinum complexes of the type [Pt(DMSO)(L)Cl]Cl, in which L represents a fluoroquinolone, namely, ciprofloxacin (cpl), ofloxacin (ofl), or sparfloxacin (spf). The new complexes were characterized by elemental analysis, high-resolution mass spectrometry (HRESIMS) and ¹H, ¹³C and ¹⁹⁵Pt NMR (nuclear magnetic resonance). The spectral data suggest that the fluoroquinolones act as bidentate ligands coordinated to Pt(II) through the nitrogen atoms of the piperazine ring. Microbiological assays against wild type Mycobacterium tuberculosis (ATCC 27294) showed that all complexes have been very potent, exhibiting antitubercular potency at concentrations <2 μM, although none of the complexes presented higher potency than established anti-TB drugs. As to the resistant strains, the complex with sparfloxacin, [Pt(DMSO)(spf)Cl]Cl exhibited the best potential against most Mycobacterium tuberculosis clinical isolates. The cytotoxicity of these compounds was also evaluated in three breast cell lines: MCF-10 (a healthy cell), MCF-7 (a hormone responsive cancer cell) and MDA-MB-231 (triple negative breast cancer cell). In both tumor cell lines, [Pt(DMSO)(spf)Cl]Cl was more active and more selective than cisplatin. Flow cytometry analysis revealed that [Pt(DMSO)(spf)Cl]Cl induced late apoptotic cell death in MDA-MB-231 cells.

这项工作描述了[Pt（DMSO）（L）Cl] Cl类型的三种铂配合物的合成，表征和生物学评估，其中L代表氟喹诺酮，即环丙沙星（cpl），氧氟沙星（ofl）或司帕沙星（spf）。通过元素分析，高分辨率质谱（HRESIMS）以及¹ H，¹³ C和¹⁹⁵ Pt NMR（核磁共振）对新配合物进行了表征。光谱数据表明，氟喹诺酮类是通过哌嗪环的氮原子与Pt（II）配位的二齿配体。针对野生型结核分枝杆菌的微生物学检测（ATCC 27294）显示，所有复合物都非常有效，在浓度小于2μM时显示出抗结核药效价，尽管没有一种复合物比已建立的抗结核药物具有更高的效价。至于耐药菌株，与司帕沙星[Pt（DMSO）（spf）Cl] Cl的复合物对大多数结核分枝杆菌临床分离株表现出最好的潜力。还在三种乳腺癌细胞系中评估了这些化合物的细胞毒性：MCF-10（健康细胞），MCF-7（激素反应性癌细胞）和MDA-MB-231（三阴性乳腺癌细胞）。在两种肿瘤细胞系中，[Pt（DMSO）（spf）Cl] Cl比顺铂更具活性，更具选择性。流式细胞仪分析表明[Pt（DMSO）（spf）Cl] Cl诱导了MDA-MB-231细胞中晚期凋亡细胞的死亡。