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Ruthenium arene complexes as HIV-1 integrase strand transfer inhibitors

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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DOI: 10.1016/j.jinorgbio.2012.09.021

Abstract

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.

Item Type:Article
ID Code:8590
Status:Published
Refereed:Yes
Uncontrolled Keywords:HIV integrase, strand transfer inhibitor, metal complex, Ru complex
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Elsevier Science
ISSN:0162-0134
Deposited On:01 Feb 2013 13:32

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