Ruthenium arene complexes as HIV-1 integrase strand transfer inhibitors
Copyright policy )Ruthenium arene complexes as HIV-1 integrase strand transfer inhibitors
The quinolone HL(1) and the hydroxypyrimidine-carboxamide HL(2) were designed and synthesized as models of the HIV integrase strand transfer inhibitors Elvitegravir and Raltegravir (brand name Isentress), with the aim to study their complexing behavior and their biological activity. The Ru(arene) complexes [RuCl(η(6)-p-cym)L(1)], [RuCl(η(6)-p-cym)L(2)] and [RuCl(hexamethylbenzene)L(2)] were also synthesized and spectroscopically characterized and their X-ray diffraction structures were discussed. The ligands and the complexes showed inhibition potency in the sub/low-micromolar concentration range in anti-HIV-1 integrase enzymatic assays, with selectivity toward strand transfer catalytic process, without any significant cytotoxicity on cancer cells.
- University of California System United States
- University of Parma Italy
- UNIVERSITY OF SOUTHERN CALIFORNIA United States
- University of Sassari Italy
Models, Molecular, Base Sequence, Molecular Mimicry, Molecular Conformation, Antineoplastic Agents, HIV Integrase, Quinolones, Crystallography, X-Ray, Pyrrolidinones, Ruthenium, Coordination Complexes, Cell Line, Tumor, Raltegravir Potassium, DNA, Viral, HIV-1, MCF-7 Cells, Organometallic Compounds, Humans, HIV Integrase Inhibitors, Cell Proliferation
Models, Molecular, Base Sequence, Molecular Mimicry, Molecular Conformation, Antineoplastic Agents, HIV Integrase, Quinolones, Crystallography, X-Ray, Pyrrolidinones, Ruthenium, Coordination Complexes, Cell Line, Tumor, Raltegravir Potassium, DNA, Viral, HIV-1, MCF-7 Cells, Organometallic Compounds, Humans, HIV Integrase Inhibitors, Cell Proliferation
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