CASDKP

Synthesis of Diketopiperazine Based Bioactive Compounds via Palladium Catalyzed Cascade Alkynylation Reactions

 Coordinatore ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE 

 Organization address address: BATIMENT CE 3316 STATION 1
city: LAUSANNE
postcode: 1015

contact info
Titolo: Prof.
Nome: Jérôme
Cognome: Waser
Email: send email
Telefono: +41 21 693 93 88
Fax: +41 21 693 97 00

 Nazionalità Coordinatore Switzerland [CH]
 Totale costo 192˙622 €
 EC contributo 192˙622 €
 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-2012-IIF
 Funding Scheme MC-IIF
 Anno di inizio 2013
 Periodo (anno-mese-giorno) 2013-04-01   -   2015-03-31

 Partecipanti

# participant  country  role  EC contrib. [€] 
1    ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE

 Organization address address: BATIMENT CE 3316 STATION 1
city: LAUSANNE
postcode: 1015

contact info
Titolo: Prof.
Nome: Jérôme
Cognome: Waser
Email: send email
Telefono: +41 21 693 93 88
Fax: +41 21 693 97 00

CH (LAUSANNE) coordinator 192˙622.20

Mappa


 Word cloud

Esplora la "nuvola delle parole (Word Cloud) per avere un'idea di massima del progetto.

bacterial    series    drug    cascade    natural    cell    derivatives    chemistry    sensing    synthesized    synthesis    newly    reaction    drugs    chemical    analogs    quorum    anticancer    diketopiperazine   

 Obiettivo del progetto (Objective)

'More than 50% of drugs currently on the market are either natural product inspired derivatives or natural products. Despite this remarkable feat, the pharmaceutical industry has partly abandoned this traditional method of drug discovery resulting in a decline of newly approved drugs. In this context, we propose the development of a novel Pd-catalyzed cascade reaction to gain highly efficient entry into the diketopiperazine framework. Using this newly developed chemical tool, analogs of natural products with confirmed quorum sensing or anticancer properties will be synthesized. Quorum sensing represents a novel therapeutic target to fight bacteria, which is especially attractive in light of the ever-expanding bacterial drug resistance, as it is based on bacterial cell-to-cell signaling disruption. Thus, we propose the synthesis of a series of diketopiperazine derivatives, based on the structure of known diketopiperazine based natural quorum sensing modulators. This task will additionally result in the implementation of a biological screening subunit within the host group. Furthermore, we aim to utilize the cascade reaction to access a series of tryprostatin A and B analogs (promising anticancer agents). A highly convergent approach is proposed herein, allowing for the synthesis of these chemical entities in half as many steps in comparison to the current “state-of-the-art” method. The synthesized derivatives will be assessed for their anticancer activity in collaboration with leading experts of the field. Thus, the proposed project entails a multidisciplinary, trans-national effort to find novel potent bioactive compounds that will certainly represent a high-quality contribution to advance the fields of Organic Chemistry, Medicinal Chemistry, Biology and Microbiology with a sustained positive impact on overall public health and welfare.'

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