PHOTO-CYCLE · Photocatalysis in Drug Discovery - Asymmetric Preparation of Bioactive Chiral Lactones and Cyclohexanols
Horizon 2020 — Marie Skłodowska-Curie Actions
- Duration
- 2020-03-01 → 2022-02-28
- EU contribution
- €160,932
- Participants
- 1
- Scheme
- MSCA-IF
Lines connect the coordinator with its partners.
Results in brief
Photocatalysis in Drug Discovery - Asymmetric Preparation of Bioactive Chiral Lactones and Cyclohexanols
Drug discovery must identify successful lead candidates. The growing perception is that basic, fundamental 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 of optimal chiral molecules that increase the probability of success in identifying drug-candidate structures. Experience shows that successful programs for drug discovery often rely on the screening of natural-like compounds. As recent statistics indicate, more than 50% of the therapeutic agents approved between 1981 and 2011 are natural or natural-like products. The proposed research aims to develop conceptually innovative, catalytic, and cost-effective methods to rapidly generate, in one single step, architecturally complex chiral natural-like compounds based on these privileged skeletons. We have pursued the PHOTO-CYCLE project under the guiding principle that compound development should be driven by discoveries and innovation in chemical methodology, providing real benefits to society through the discovery of new therapeutics. Additionally, the use of visible light to drive the chemical transformations involved in the project provide high environmental benefits. The resulting synthetic platform will be used as an ideal starting point for assembling libraries featuring biologically privileged scaffolds. These scaffolds will comprise chiral polycyclic lactones and polyfunctionalized cyclohexanols, which, along with biological screening, will increase the probability of success in identifying drug-candidate structures. Emphasis will be put on the importance of developing chemical methodology to lactones and polyfunctionalized cyclohexanols, its application towards drug synthesis, and environmental benefit of using visible light to drive chemical processes. The goal of our research is to combine the potential of asymmetric organocatalysis and photocatalysis, two powerful fields of molecule activation, to design novel cascade reactions.
Data: CORDIS, © European Union
Project objective
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 of optimal chiral molecules that increase the probability of success in identifying drug-candidate structures. PHOTO-CYCLE seeks to provide some solutions by developing effective technology to rapidly generate, in one single step, architecturally complex chiral natural-like compounds. Specifically, we will use photochemical organocatalytic cascade processes to synthesise polycyclic lactones and polyfunctionalized cyclohexanols, which are common motifs in biologically active molecules. We will combine asymmetric organocatalysis and photochemistry, two powerful strategies of modern chemical research. They have extraordinary potential for the sustainable preparation of novel organic molecules, which are needed to drive innovation in the pharmaceutical industry. PHOTO-CYCLE aims to combine the fellow’s experience in allene chemistry and organocatalysis and the host’s experience in photo-triggered asymmetric processes to develop otherwise unachievable catalytic asymmetric cascade reactions. Specifically, we will focus on the rich reactivity of excited chiral iminium ions to activate readily available allenes and trigger cascade processes. The resulting strategies will be used as an ideal platform for assembling libraries comprising chiral polycyclic lactones and cyclohexanols, which, along with biological screening carried out in collaboration with Lundbeck A/S, will increase the probability of success in identifying drug-candidate structures. The multi-cultural and intersectorial nature of this project will greatly contribute to broaden the fellow’s competencies and will place him in a competitive position for the next career move.
Original text from CORDIS.
Participants
- FUNDACIO INSTITUT CATALA D'INVESTIGACIO QUIMICA · TARRAGONACoordinatorSpain
Links
Data: CORDIS, © European Union