Specific and enantioselective sulfoxidation of an aryl-trifluoromethylsulfide by rat liver cytochromes P-450

International audienc

Semisynthesis of (+)- and (?)-goniomitine from (?)- and (+)-vincadifformine

International audienc

Bis-macrocyclic diketal diamines, analogue of the anti-viral and anti-tumoral bicyclam AMD 3100

Poste

First-in-class combination therapy of a copper(II) metallo-phosphorus dendrimer with cytotoxic agents

International audienceThe metallo-phosphorus dendrimer 1G3-Cu (generation 3 dendrimer bearing 48 conjugated copper(II) on its surface) has antiproliferative activity related to its capacity to activate Bax translocation. In the present study, we evaluate the activity of an association of 1G3-Cu with 5 cytotoxic agents used in chemotherapy having different modes of action. Data show no additive effect with camptothecin and cisplatin, additivity with paclitaxel and MG132, and synergy with doxorubicin. Results suggest that the multivalent Cu-conjugated dendrimer 1G3-Cu (activator of Bax translocation) plays an important role in boosting the clinical impact of Bax accumulation stimulated by the proteasome inhibitor MG132, antimitotic taxanes, and the topo II inhibitor doxorubicin

Synthesis and anti-proliferative activity of novel quinolin-8-ol derivatives

International audienc