Synthesis of naphthopyrrolo[3,4-c]carbazoles

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Synthesis and Reactivity of 7-Azaindole (1H-Pyrrolo[2,3-b]pyridine)

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Synthesis of benzo analogs of oxoarcyriaflavins and caulersine

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Recent advances in the synthesis and properties of 4-, 5-, 6- or 7-azaindoles

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Potassium [1-(tert-Butoxycarbonyl)-1H-indol-2-yl]trifluoroborate as an Efficient Building Block in Palladium-Catalyzed Suzuki-Miyaura Cross Couplings

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Synthesis of new fused and substituted benzo and pyrido carbazoles via C-2 (het)arylindoles

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The Azaindole Framework in the Design of Kinase Inhibitors

This review article illustrates the growing use of azaindole derivatives as kinase inhibitors and their contribution to drug discovery and innovation. The different protein kinases which have served as targets and the known molecules which have emerged from medicinal chemistry and Fragment-Based Drug Discovery (FBDD) programs are presented. The various synthetic routes used to access these compounds and the chemical pathways leading to their synthesis are also discussed. An analysis of their mode of binding based on X-ray crystallography data gives structural insights for the design of more potent and selective inhibitors

Comparison of the efficiencies of two TR-FRET methods to detect in vitro natural and synthesized inhibitors of the Raf/MEK/ERK signaling pathway

International audienceNumerous types of cancer operate through the deregulation of the Raf/MEK/ERK pathway. It is therefore of importance to design and synthesize inhibitors of this pathway. Consequently, we have developed several tests to measure in vitro the effect of inhibitors on the activity of the complete cascade Raf-1/MEK/ERK and also on the activities of Raf-1, MEK, and ERK individually. We present here the results obtained with two time-resolved fluorescence resonance energy transfer (TR-FRET) methods by comparison with a classical radioactivity method and experimental data found in literature. The capability of a series of optimized assays to detect different types of inhibitors is evaluated and discussed. Keywords: Raf/MEK/ERK cascade, inhibitors of Raf-1, MEK, and ERK, PEBP/RKIP, phosphocellulose filter binding assay, time-resolved fluorescence resonance energy transfe

A mild and selective method for N-Boc deprotection

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