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Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors
Authors:Suvi Rajamaki  Anna Innitzer  Chiara Falciani  Cristina Tintori  Frauke Christ  Myriam Witvrouw  Zeger Debyser  Silvio Massa  Maurizio Botta
Institution:1. Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, Via A. De Gasperi 2, I-53100 Siena, Italy;2. Molecular Medicine, Katholieke Universiteit Leuven, Kapucijnenvoer 33, B-3000 Leuven, Flanders, Belgium
Abstract:A novel compound inhibiting HIV-1 integrase has been identified by means of virtual screening techniques. A small family of structurally related molecules has been synthesized and biologically evaluated with some of the compounds possessing micromolar activity both in enzymatic and cellular assays.
Keywords:
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