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Dr. Luca Sancineto, Dr. Nunzio Iraci, Dr. Serena Massari, Dr. Vanessa Attanasio, Dr. Gianmarco Corazza, Dr. Maria Letizia Barreca, Dr. Stefano Sabatini, Dr. Giuseppe Manfroni, Dr. Nilla Roberta Avanzi, Prof. Violetta Cecchetti, Prof. Christophe Pannecouque, Prof. Alessandro Marcello and Dr. Oriana Tabarrini Computer-Aided Design, Synthesis and Validation of 2-Phenylquinazolinone Fragments as CDK9 Inhibitors with Anti-HIV-1 Tat-Mediated Transcription Activity ChemMedChem 8

Version of Record online: 21 OCT 2013 | DOI: 10.1002/cmdc.201300287

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Potent fragments! A 2-phenylquinazolinone fragment was initially identified by computational study, which after a first optimization evolved into a series of compounds capable of inhibiting cyclin-dependent kinase 9 (CDK9) activity at micromolar concentrations. The anti-kinase activity translated well into the ability to inhibit Tat-mediated transcription and HIV-1 infectivity in latently infected cells.

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