ELECTROINDOLE

Electrophilic Indoles for the Enantioselective Synthesis of Benzofuroindolines related to Diazonamide A

 Coordinatore UNIVERSITE PARIS-SUD 

 Organization address address: RUE GEORGES CLEMENCEAU 15
city: ORSAY
postcode: 91405

contact info
Titolo: Mr.
Nome: Nicolas
Cognome: Lecompte
Email: send email
Telefono: +331 69 15 55 89

 Nazionalità Coordinatore France [FR]
 Totale costo 194˙046 €
 EC contributo 194˙046 €
 Programma FP7-PEOPLE
Specific programme "People" implementing the Seventh Framework Programme of the European Community for research, technological development and demonstration activities (2007 to 2013)
 Code Call FP7-PEOPLE-2013-IIF
 Funding Scheme MC-IIF
 Anno di inizio 2015
 Periodo (anno-mese-giorno) 2015-02-19   -   2017-02-18

 Partecipanti

# participant  country  role  EC contrib. [€] 
1    UNIVERSITE PARIS-SUD

 Organization address address: RUE GEORGES CLEMENCEAU 15
city: ORSAY
postcode: 91405

contact info
Titolo: Mr.
Nome: Nicolas
Cognome: Lecompte
Email: send email
Telefono: +331 69 15 55 89

FR (ORSAY) coordinator 194˙046.60

Mappa


 Word cloud

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clinical    synthesis    phenols    benzofuroindolines    indoles    library    analogs    diazonamide    natural    reactions    cell    benzofuroindoline    lines    cancer    eacute    enantioselective   

 Obiettivo del progetto (Objective)

'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.'

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