Antiproliferative activity of dmoPTA–Ru(II) complexes against human solid tumor cells

• Published in: Bioorganic & medicinal chemistry letters 2011-08, Vol.21 (15), p.4568-4571
• Main Authors: Ríos-Luci, Carla, León, Leticia G., Mena-Cruz, Adrián, Pérez-Roth, Eduardo, Lorenzo-Luis, Pablo, Romerosa, Antonio, Padrón, José M.
• Format: Article
• Language: English
• Subjects: Antineoplastic agents; Antineoplastic Agents - chemistry; Antineoplastic Agents - therapeutic use; Antineoplastic Agents - toxicity; Antitumor drugs; bioactive properties; Biological and medical sciences; cell cycle; Cell cycle arrest; Cell Line, Tumor; cisplatin; Coordination Complexes - chemistry; Coordination Complexes - therapeutic use; Coordination Complexes - toxicity; DNA; Drug Screening Assays, Antitumor; General aspects; Humans; Hydrosoluble phosphines; Medical sciences; Neoplasms - drug therapy; Organometallic drugs; Pharmacology. Drug treatments; Ruthenium - chemistry; Ruthenium complexes
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2011.05.116

[Display omitted] 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.