Departamento de Química, Facultad de Ciencias, Universidad de Burgos, Plaza Misael Bañuelos s/n, 09001, Burgos, Spain.
Inorg Chem. 2020 Apr 6;59(7):4961-4971. doi: 10.1021/acs.inorgchem.0c00219. Epub 2020 Mar 17.
A new family of neutral chiral cyclometalated platinum(II) complexes with formula [Pt(κ-())Cl(κ-())], where () = 2-phenylpyridinate and () = 2-(2-pyridyl)benzimidazole () or (N-(CH)--(2-(2-pyridyl)benzimidazole) ligands; ( = phenyl (), naphthyl (), pyrenyl ()), have been synthesized and completely characterized. The unexpected κ coordination mode of the 2-(2-pyridyl)benzimidazole-derived ligands has been confirmed by spectroscopic techniques and X-ray diffraction. The aromatic moieties on the ligands in the new platinum(II) complexes have a remarkable influence on the cytotoxicity and in the binding mode to DNA. complexes internalized more than cisplatin in the SW480 cancer cells even though only and display high cytotoxicity. H NMR and P{H}NMR pointed out that and complexes bind covalently to GMP, while the electrophoresis assays and CD experiments indicate that only is able to covalently interact with DNA, inducing the same conformational changes in the plasmid DNA as cisplatin. Although the complex intercalates into DNA, probably through the pyrenyl moiety, no biological activity is observed.
一类新的中性手性环金属化铂（II）配合物，其通式为[Pt(κ-())Cl(κ-())]，其中()= 2-苯基吡啶并[2,3-d]嘧啶和()= 2-(2-吡啶基)苯并咪唑()或 (N-(CH)--(2-(2-吡啶基)苯并咪唑)配体；()= 苯基()、萘基()、芘基()），已经被合成并进行了完全的表征。通过光谱技术和 X 射线衍射证实了来自 2-(2-吡啶基)苯并咪唑的配体的预期κ配位模式。在新的铂（II）配合物中，配体上的芳基部分对细胞毒性和与 DNA 的结合模式有显著的影响。尽管只有 和 表现出高的细胞毒性，但 复合物在 SW480 癌细胞中的内化程度超过了顺铂。1H NMR 和 31P{1}H NMR 表明 和 复合物以共价键结合到 GMP，而电泳分析和 CD 实验表明，只有 能够与 DNA 发生共价相互作用，诱导与顺铂相同的质粒 DNA 构象变化。尽管复合物 可能通过芘基部分插入 DNA，但没有观察到生物活性。
