A Photochemical Approach to Pyridopyrroloquinoline Derivatives as New Potential Anticancer Agents

International audienceIndoloquinoline alkaloid cryptolepine and pyridocarbazole alkaloid ellipticine are of great interest becausein vitro and in vivo studies revealed their good cytotoxic properties. In order to obtain some biologically activeanalogs of these compounds, we developped a synthesis based on the photocyclisation of tertiary N-methylatedenaminones derived from cyclopentane-1,3-dione and 3 or 6-aminoquinoline. The angular cyclised compoundsthus obtained were submitted to Beckmann rearrangement, preceded by the formation of a Z oxime. Finally, thed -lactame ring was oxidized using 10% palladium/carbon in diphenylether and pyridopyrroloquinolines wereobtained. These compounds and the intermediate lactams and cyclopentanopyrroloquinolines were tested in vitroon K 562 cells and A 2780 doxorubicine sensitive and resistant cells. All compounds were less effective than doxorubicine in sensitive cells but their activity wasn’t decreased by MDR resistance

Synthesis and in Vitro Cytotoxic Evaluation of New Derivatives of Pyrido[1,2-a]benzimidazolic Ring System: The Pyrido[1,2:1,2]imidazo[4,5-h]quinazolines

International audienceAccess to the original series of pyrido[1',2':1,2]imidazo[4,5-h]quinazoline was developed from a 1,3-dicarbonyl unit with some “N-C-N” bisnucleophilic reagents and the derivatives obtained were evaluated for in vitro cytotoxic activities against HL60 and A2780 cells. All compounds exhibited cytotoxic activitise on resistant cell lines (MDR+; HL60R and A2780R) with no resistance phenomena

An Ethernet motion-sensor based alarm system for epilepsy monitoring

International audienceThe EPIMOUV project aims at providing a place to live and autonomy for drug-resistant epileptic young adults while attempting to provide them a high level of security. In this framework, subjects will be monitored during night using body-worn motion sensors and an alarm will be triggered if an on-going seizure is detected by processing the accelerometer readings. In this paper, we describe an innovative architecture for such alarm system: the wireless inertial sensors are positioned on the subject's body; the RF transceiver is located in the subject's room and linked to an Ethernet gateway, and the remote motion capture acquisition system is interfaced with a medicalized alarm system. The EPIMOUV system will be evaluated in a specialized institution from December 2010.L’objectif global du projet EPIMOUV est d’augmenter l’autonomie des personnes souffrant d’une épilepsie pharmaco-résistante tout en préservant leur sécurité. Pour cela, le projet vise à développer un système d’alarme en cas de crise épileptique nocturne par analyse du mouvement. Dans ce papier, nous décrivons une architecture innovante de système d’alarme médicalisé : les accéléromètres sans fil sont placés sur le corps ; le récepteur RF est situé dans la chambre du résident et relié au réseau par connexion Ethernet ; et le système déporté d’acquisition de capture de mouvement et de détection de crises est interfacé à un système professionnel d’alarme médicalisé. Le système EPIMOUV sera évalué en institution spécialisé à partir de décembre 2010