bis(S-Acyl-2-thioethyl)esters of 2′,3′-Dideoxyadenosine 5′-Monophosphate Are Potent Anti-HIV Agents in Cell Culture

C. Périgaud Laboratoire de Chimie Bio-Organique, U. R. A. 488 du C. N. R. S., Université Montpellier II, Case Courrier 008 Place Eugégne Bataillon, 34095, Montpellier Cédex, 5, France

G. Gosselin Laboratoire de Chimie Bio-Organique, U. R. A. 488 du C. N. R. S., Université Montpellier II, Case Courrier 008 Place Eugégne Bataillon, 34095, Montpellier Cédex, 5, France

S. Benzaria Laboratoire de Chimie Bio-Organique, U. R. A. 488 du C. N. R. S., Université Montpellier II, Case Courrier 008 Place Eugégne Bataillon, 34095, Montpellier Cédex, 5, France

J.-L. Girardet Laboratoire de Chimie Bio-Organique, U. R. A. 488 du C. N. R. S., Université Montpellier II, Case Courrier 008 Place Eugégne Bataillon, 34095, Montpellier Cédex, 5, France

G. Maury Laboratoire de Chimie Bio-Organique, U. R. A. 488 du C. N. R. S., Université Montpellier II, Case Courrier 008 Place Eugégne Bataillon, 34095, Montpellier Cédex, 5, France

H. Pélicano Laboratoire de Chimie Bio-Organique, U. R. A. 488 du C. N. R. S., Université Montpellier II, Case Courrier 008 Place Eugégne Bataillon, 34095, Montpellier Cédex, 5, France

A.-M. Aubertin Université Louis Pasteur, I. N. S. E. R. M. U, 74, 3 Rue Koeberlé, 67000, Strasbourg, France

A. Kirn Université Louis Pasteur, I. N. S. E. R. M. U, 74, 3 Rue Koeberlé, 67000, Strasbourg, France

J.-L. Imbach Laboratoire de Chimie Bio-Organique, U. R. A. 488 du C. N. R. S., Université Montpellier II, Case Courrier 008 Place Eugégne Bataillon, 34095, Montpellier Cédex, 5, France

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Abstract

It is shown that ddA bis(SATE)phosphotriesters have potent anti-HIV activity in cell culture. Thus, compared with the parent nucleoside, a decrease of 3 or 4 orders of magnitude was observed in the EC₅₀ values for the bis(S-acetyl-2-thioethyl)phosphotriester derivative, which makes this compound as active as AZT.

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bis(S-Acyl-2-thioethyl)esters of 2′,3′-Dideoxyadenosine 5′-Monophosphate Are Potent Anti-HIV Agents in Cell Culture

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bis(S-Acyl-2-thioethyl)esters of 2′,3′-Dideoxyadenosine 5′-Monophosphate Are Potent Anti-HIV Agents in Cell Culture

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