ORGANO-GOLD CAT | Merging organo- and gold-catalysis to design cascade reactions: a shortcut toward molecular complexity

Summary
We are in a changing era for drug discovery: the growing perception is that basic chemical research will play a greater role in pharmaceutical development. One current challenge is to develop a new kind of chemistry that yields a screening collection comprising optimal chiral molecules that increase the probability of success in identifying drug-candidate structures. The proposed research aims to develop conceptually innovative catalytic methods to rapidly generate, in one single step, architecturally complex chiral natural-like compounds. Natural products have been selected in evolution and their underlying structural scaffolds define biologically relevant fractions of chemical space. Consequently, compound libraries inspired by natural structures deliver lead candidates with a higher hit-rate than conventional lead generation strategies.

We will pursue the proposed research project under the guiding principle that compound development should be driven by discoveries and innovation in chemical methodology. The goal of the research project is to combine the potential of asymmetric organocatalysis and gold catalysis, powerful fields of molecule activation, to find cost-effective synthetic methods for reproducing the rich structural diversity of natural molecules. Since the vast majority of natural products and drug-like compounds possess heterocyclic moieties, we will focus on preparing diverse heterocyclic compounds, especially based on the furan unit. The resulting synthetic platform will be used as an ideal starting point for assembling enantiopure chiral 2,3-furan fused carbocycles, which, along with biological screening carried out in collaboration with a world-wide recognized pharma-company (Lundbeck A/S), will increase the probability of success in identifying drug-candidate structures. The multi-cultural nature of this project will greatly contribute to broaden the fellow competencies and will place him in an excellent position for the next career move
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More information & hyperlinks
Web resources: https://cordis.europa.eu/project/id/658980
Start date: 01-06-2015
End date: 31-05-2017
Total budget - Public funding: 158 121,60 Euro - 158 121,00 Euro
Cordis data

Original description

We are in a changing era for drug discovery: the growing perception is that basic chemical research will play a greater role in pharmaceutical development. One current challenge is to develop a new kind of chemistry that yields a screening collection comprising optimal chiral molecules that increase the probability of success in identifying drug-candidate structures. The proposed research aims to develop conceptually innovative catalytic methods to rapidly generate, in one single step, architecturally complex chiral natural-like compounds. Natural products have been selected in evolution and their underlying structural scaffolds define biologically relevant fractions of chemical space. Consequently, compound libraries inspired by natural structures deliver lead candidates with a higher hit-rate than conventional lead generation strategies.

We will pursue the proposed research project under the guiding principle that compound development should be driven by discoveries and innovation in chemical methodology. The goal of the research project is to combine the potential of asymmetric organocatalysis and gold catalysis, powerful fields of molecule activation, to find cost-effective synthetic methods for reproducing the rich structural diversity of natural molecules. Since the vast majority of natural products and drug-like compounds possess heterocyclic moieties, we will focus on preparing diverse heterocyclic compounds, especially based on the furan unit. The resulting synthetic platform will be used as an ideal starting point for assembling enantiopure chiral 2,3-furan fused carbocycles, which, along with biological screening carried out in collaboration with a world-wide recognized pharma-company (Lundbeck A/S), will increase the probability of success in identifying drug-candidate structures. The multi-cultural nature of this project will greatly contribute to broaden the fellow competencies and will place him in an excellent position for the next career move

Status

CLOSED

Call topic

MSCA-IF-2014-EF

Update Date

28-04-2024
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Horizon 2020
H2020-EU.1. EXCELLENT SCIENCE
H2020-EU.1.3. EXCELLENT SCIENCE - Marie Skłodowska-Curie Actions (MSCA)
H2020-EU.1.3.2. Nurturing excellence by means of cross-border and cross-sector mobility
H2020-MSCA-IF-2014
MSCA-IF-2014-EF Marie Skłodowska-Curie Individual Fellowships (IF-EF)