- Identification of novel microsomal prostaglandin E2synthase-1 (mPGES-1) lead inhibitors from Fragment Virtual Screening
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Identification of new microsomal prostaglandin E2synthase-1 (mPGES-1) inhibitors is currently sought for the treatment of cancer and inflammation. Here we show the results of a Fragment Virtual Screening campaign using the X-ray crystal structu
- Lauro, Gianluigi,Manfra, Michele,Pedatella, Silvana,Fischer, Katrin,Cantone, Vincenza,Terracciano, Stefania,Bertamino, Alessia,Ostacolo, Carmine,Gomez-Monterrey, Isabel,De Nisco, Mauro,Riccio, Raffaele,Novellino, Ettore,Werz, Oliver,Campiglia, Pietro,Bifulco, Giuseppe
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- Preparation of 6-, 7-, and 8-substituted derivatives of 2-oxa-1,3,4,10-tetraazacyclopenta[b]fluoren-9-one
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The preparation of a variety of derivatives of 2-oxa-1,3,4,10-tetraazacyclopenta[b]fluoren-9-one 1 is described. A series of substituted indan-1-ones were prepared and oxidized with N-bromosuccinimide and dimethyl sulfoxide to the corresponding ninhydrin derivatives. Cyclization of the ninhydrins with furazan-3,4-diamine yielded the target tetracycles. Appropiate choice of substituents in ninhydrins led to a preference for one regioisomer in the target tetracycles. This permitted the synthesis of a variety of 8-substituted heterocycles. In those instances where isomer formation was possible, structural assignments were confirmed by X-ray crystallography.
- Bratton,Unangst,Rubin,Trivedi
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p. 1103 - 1111
(2007/10/03)
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