62 research outputs found
5‐Imidazolyl‐quinolinones, ‐quinazolinones and ‐benzo‐azepinones as Farnesyltransferase Inhibitors.
No full textSubstituted Azoloquinolines and ‐quinazolines as New Potent Farnesyl Protein Transferase Inhibitors.
No full text4‐Methyl‐1,2,4‐triazol‐3‐yl Heterocycle as an Alternative to the 1‐Methylimidazol‐5‐yl Moiety in the Farnesyltransferase Inhibitor ZARNESTRA.
No full textAuthor Correction: Structural basis of astrocytic Ca2+ signals at tripartite synapses (Nature Communications, (2020), 11, 1, (1906), 10.1038/s41467-020-15648-4)
No full textAn amendment to this paper has been published and can be accessed via a link at the top of the paper
Towards New Sila- or Germa-Derivatives of Motesanib
No full textInternational audienceDeveloping new access to original silylated heterocycles is an emerging challenge in medicinal chemistry. In this paper, we describe a synthesis of silylated and germylated Motesanib analogues relying on a peptide coupling between a nicotinic acid derivative and silylated or germylated heterocycles, prepared according to our previous reports
Access to Silylated Pyrazole Derivatives by Palladium-Catalyzed C−H Activation of a TMS group
No full textInternational audienceA simple and efficient approach to new silylated heterocycles of potential interest in medicinal chemistry is presented. A set of bromophenyl trimethylsilyl pyrazole intermediates can be transformed by direct organometallic routes into two families of regioisomeric iodoaryl substrates; using either arylzinc or aryllithium chemistry, the TMS group remains on the pyrazole ring or translocates to the aryl moiety. These two families can then be efficiently transformed into benzo silino pyrazoles thanks to a single‐step cyclization relying on the Pd‐catalyzed activation of a non‐activated C(sp3)−H bond alpha to a silicon atom. The experimental conditions used, which are fully compatible with the pyrazole ring, suggest that this reaction evolves through a concerted metalation–deprotonation (CMD) mechanism
Abstract LB-233: Unique physicochemical properties of the potent FGFR 1, 2, 3 and 4 inhibitor JNJ-42756493 contribute to prolonged target shutdown
No full textTandem Suzuki-Miyaura Coupling/Acid-Catalyzed Cyclization between Vinyl Ether Boronates and Vinyl Halides: A Concise Approach to Polysubstituted Furans
No full textInternational audiencePolysubstituted 2-(ω-hydroxyalkyl)furans were prepared by tandem Suzuki-Miyaura coupling/acid-catalyzed cyclization starting from appropriately substituted 3-haloallylic alcohols and dihydrofuran-, dihydropyran-or glycal-derived pinacol boronates
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