BioLab, Instituto Universitario de Bio-Orgánica Antonio González (IUBO-AG), Universidad de La Laguna, La Laguna, Spain.
Bioorg Med Chem Lett. 2011 Aug 1;21(15):4568-71. doi: 10.1016/j.bmcl.2011.05.116. Epub 2011 Jun 12.
The biological evaluation of new Ru(II) complexes carrying dmoPTA (dmoPTA=3,7-dimethyl-1,3,7-triaza-5-phosphabicyclo[3.3.1]nonane) ligands is reported. The results on the biological activity revealed that the organometallic complexes are active against all cell lines with GI(50) values in the range 1.1-2.6 μM. When compared to the standard anticancer drug cisplatin, the bimetallic Ru(II) complexes showed a greater activity profile. The cell cycle analysis revealed that the new compounds induced arrest in G(1) phase. Contrary to cisplatin, these Ru(II) complexes do not interact with DNA. This result suggests that DNA might not be the key pharmacological target.
报告了新型 Ru(II) 配合物携带 dmoPTA（dmoPTA=3,7-二甲基-1,3,7-三氮杂-5-磷杂环戊烷）配体的生物学评价。生物活性结果表明，这些有机金属配合物对所有细胞系均具有活性，GI（50）值在 1.1-2.6 μM 范围内。与标准抗癌药物顺铂相比，双金属 Ru(II) 配合物显示出更大的活性谱。细胞周期分析表明，新化合物诱导 G1 期停滞。与顺铂相反，这些 Ru(II) 配合物不与 DNA 相互作用。这一结果表明，DNA 可能不是关键的药理靶标。
