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Séminaire Chimie ED459

Organometallic catalysis (silver, rhodium and cobalt) for the access to heterocycles – an approach for silicon-containing cyclopenta[c]acridine derivatives as kinases inhibitors

Prof. Philippe Belmont (Faculté de Pharmacie, Université Paris-Descartes)

publié le

Le Jeudi 04 juin 2015 à 13h45
UM FdS, salle de cours SC-20.02

[la conférence sera présentée en français]

Our field of interest and expertise are in organometallic chemistry (Au, Ag, Co, Rh) devoted to the original access to various heterocyclic structures in view of studying their biological properties, in particular against tumors (e.g. kinases inhibition).
Indeed, we develop methods for the access to various heterocycles of broad biological interest, such as quinolines (and derivatives), acridines, dibenzofurans and carbazoles, using metal-free or metal-catalyzed reactions. For instance, furoquinoline and pyranoquinoline cores, structurally related to known alkaloids, can be easily accessed via a tandem acetalization/cycloisomerization reaction with a broad scope, using gold salts or various silver salts. Also, various spirocyclic structures can be obtained through [4+2] or [3+2] cycloaddition reactions onto furoquinoline derivatives. Finally, 1H,1-arylisochomenes can also be easily obtained under silver-catalysed cyclofunctionalization reactions.

Moreover, we are developing a new heterocycle family, cyclopenta[c]acridinones, exhibiting exquisite biological properties (collaboration Dr. L. Meijer). Indeed, these silicon-containing derivatives inhibit selectively cyclin-dependent kinases (CDKs) at nanomolar concentrations. Co-crystallization data are leading the design of novel inhibitors that will be discussed.

Contact local ICGM : Prof. Jean-Marc Campagne (équipe AM2N)

Voir en ligne : équipe de P. Belmont

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