Objectif The objectives of this project are the development of A new and efficient asymmetric oxidative coupling reaction between phenols and indoles for the synthesis of benzofuroindolines analogs of diazonamide A and the biological evaluation of a library of this family of compounds.The benzofuroindoline core is a unique motif found in the natural products diazonamide A, a very potent anti-cancer agent (<5 nM against various cell lines) which may have clinical utility for cancer therapy since it is as active as widespread used antimitotic drugs without their overt toxicity. Unfortunately, the known synthetic methods for the generation of the benzofuroindoline scaffold are not short, high yielding and enantioselective at the same time. Therefore, we aim to study and develop direct and general methods for the synthesis of this important pharmacophore. We desire to use as starting materials phenols and indoles that are the postulated biosynthetic precursors of the natural benzofuroindolines.To meet this goal, we propose an innovative strategy based on the scarsely known electrophilic character of the indole nucleus.We will particularly aim at the development of enantioselective catalytic reactions.After the development of suitable reactions for the synthesis of benzofuroindolines, we intend to create a library of analogs of diazonamide A that will be evaluated against different tumoral cell lines in order to discover simplified analogs which would be synthesized in few steps with retention of the clinical potential of diazonamide A.The research will be conducted at the Institut de Chimie Moléculaire et des Matériaux d’Orsay (ICMMO), Université Paris-Sud 11 by Raj Kumar Nandi under the responsability of Guillaume Vincent. Champ scientifique medical and health sciencesclinical medicineoncology Programme(s) FP7-PEOPLE - Specific programme "People" implementing the Seventh Framework Programme of the European Community for research, technological development and demonstration activities (2007 to 2013) Thème(s) FP7-PEOPLE-2013-IIF - Marie Curie Action: "International Incoming Fellowships" Appel à propositions FP7-PEOPLE-2013-IIF Voir d’autres projets de cet appel Régime de financement MC-IIF - International Incoming Fellowships (IIF) Coordinateur UNIVERSITE PARIS-SUD Contribution de l’UE € 194 046,60 Adresse RUE GEORGES CLEMENCEAU 15 91405 ORSAY CEDEX France Voir sur la carte Type d’activité Higher or Secondary Education Establishments Contact administratif Nicolas Lecompte (Mr.) Liens Contacter l’organisation Opens in new window Site web Opens in new window Coût total Aucune donnée