Carcelli, Mauro and Bacchi, Alessia and Pelagatti, Paolo and Rispoli, Gabriele and Rogolino, Dominga and Sanchez, Tino W. and Sechi, Mario and Neamati, Nouri (2013) Ruthenium arene complexes as HIV-1 integrase strand transfer inhibitors. Journal of Inorganic Biochemistry, Vol. 118 , p. 74-82. ISSN 0162-0134. Article.
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The quinolone HL1 and the hydroxypyrimidine-carboxamide HL2 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(η6-p-cym)L1], [RuCl(η6-p-cym)L2] and [RuCl(hexamethylbenzene)L2] 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.
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