Dr. Olivier Mirguet, Yann Lamotte, Chun-wa Chung, Dr. Paul Bamborough, Delphine Delannée, Dr. Anne Bouillot, Dr. Françoise Gellibert, Gael Krysa, Antonia Lewis, Dr. Jason Witherington, Pascal Huet, Yann Dudit, Dr. Lionel Trottet and Dr. Edwige Nicodeme Naphthyridines as Novel BET Family Bromodomain Inhibitors ChemMedChem 9
Version of Record online: 2 SEP 2013 | DOI: 10.1002/cmdc.201300259
Place your BET! Naphthyridine derivatives were designed and synthesized as potent inhibitors of the BET bromodomain family with good cell activity and oral pharmacokinetic parameters. X-ray crystal structures were solved and quantum mechanical calculations were used to explain the higher affinity of the 1,5-isomer over the others. The best compounds were progressed in a mice model of inflammation and exhibited dose-dependent anti-inflammatory pharmacology.
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