Conception et synthèses régiospécifiques de purines di- et trisubstituées comme inhibiteurs de la glycogène synthase kinase-3

ORSAY-PARIS 11-BU Sciences (914712101) / SudocSudocFranceF

High-Yielding Two Step Synthesis of 6,8-Disubstitued N-9-Unprotected Purines

International audienc

Synthesis of 6,7,8-Trisubstituted Purines via a Copper-Catalyzed Amidation Reaction

International audienc

Novel 8-arylated purines as inhibitors of glycogen synthase kinase

International audienc

Regioselective Sonogashira cross-coupling reactions of 6-chloro-2,8-diiodo-9-THP-9H-purine with alkyne derivatives

International audienc

Microwave-Assisted Pd/Cu-Catalyzed C-8 Direct Alkenylation of Purines and Related Azoles An Alternative Access to 6,8,9-Trisubstituted Purines

International audienc

Palladium-Catalyzed Amidation and Amination of 8-Iodopurine

International audienc

Targeting the cell cycle and the PI3K pathway: A possible universal strategy to reactivate innate tumor suppressor programmes in cancer cells

International audienc

A Pd(0) based cross-coupling approach to the synthesis of 2-amidopurines and their evaluation as CDK inhibitors.

Two new series of 2-amido- and 2-aminocarbonylpurines have been synthesized using a Pd catalyst cross-coupling reaction either with amides or amines in the presence of CO. Moderate in vitro inhibitory activity against CDK1 and CDK5 was observed with IC(50) of 0.9muM for the most active compound (18c)

Microwave-Assisted Pd/Cu-Catalyzed C-8 Direct Alkenylation of Purines and Related Azoles: An Alternative Access to 6,8,9-Trisubstituted Purines

An efficient microwave-assisted palladium/copper comediated C-8 direct alkenylation of purines with styryl bromides has been developed. The method is regioselective, functional group tolerant, rapid, and compatible with other related azoles. Combined with subsequent nucleophilic substitution, it provides an easy access to new 6,8,9-trisubstituted purines