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Polyanion Inhibitors of Human Immunodeficiency Virus and Other Viruses. 6. Micelle-like Anti-HIV Polyanionic Compounds Based on a Carbohydrate Core

1997; American Chemical Society; Volume: 40; Issue: 3 Linguagem: Inglês

10.1021/jm960348y

1520-4804

Alain Leydet, Christine Jeantet‐Segonds, Corinne Bouchitté, Céline Moullet, Bernard Boyer, Jean Pierre Roque, Myriam Witvrouw, José A. Esté, Robert Snoeck, Graciela Andreï, Erik De Clercq,

HIV Research and Treatment

A new class of polyanionic compounds, inhibitors of human immunodeficiency virus, was obtained from radical addition of mercapto acid or mercapto ester on a perallylated carbohydrate under UV irradiation with a catalytic amount of AIBN. Unlike the polyanions that we have previously prepared by polymerization reactions, the compounds are structurally well defined. Polyanions bearing 16 carboxylate groups showed a 50% inhibitory concentration (IC50) of 0.1−4.1 μg/mL against HIV-1 in MT-4 cells while not being toxic to the host cells at concentrations up to 125 μg/mL. The most potent polyanions also proved active against human cytomegalovirus at concentrations of 1−14 μg/mL. No activity was observed against any of the other viruses tested (i.e., herpes simplex virus, vesicular stomatitis virus, Sindbis, Semliki forest, parainfluenza-3, Junin, Tacaribe, Coxsackie B4, polio-1, reo-1, or vaccinia virus).