Project description
Advanced methods for modifying drug molecules
Late-stage functionalisation (LSF) is a method used to make small, specific changes to complex molecules, often near the end of their synthesis. In bioactive compounds, such as drugs, LSF enables the addition or modification of functional groups without altering the core structure. This is useful for fine-tuning the properties of a compound, saving time while improving its effectiveness or reducing side effects. With the support of the Marie Skłodowska-Curie Actions programme, the LateFun project aims to pioneer an LSF method for adding versatile functional groups to alkenes and 1,3-dienes, organic molecules with a unique structure that allows for diverse chemical reactions.
Objective
The late-stage functionalization (LSF) of bioactive compounds is currently a hot topic in the chemistry community, as it allows for the rapid and divergent construction of molecule complexity and avoids the need for time-consuming de novo synthesis. This is especially relevant in the fields of drug discovery and medicinal chemistry where the fast identification of structure-activity relationships is crucial. Especially intriguing in this context are alkenes and 1,3-dienes, as they are frequently occurring motifs in natural products and drug molecules including important antibiotics and antivirals. However, methods for the introduction of a broad variety of functional groups via the LSF of these moieties remain underdeveloped. LateFun aims to create new chemical space by developing a first-in-class methodology for the incorporation of a highly versatile functional handle via the LSF of alkenes and 1,3-dienes, whose well-established subsequent transformations will allow for the rapid assembly of diverse structures. Applying this innovative protocol to the LSF of complex natural products and drug molecules will be of great importance and impact, going beyond the current state of art. The real-life applications of this cutting-edge research proposal will be explored during a secondment phase in Novartis (Basel), providing for valuable industry insights and interdisciplinary aspects. The host’s expertise in late-stage functionalization of bioactive molecules using catalytically generated carbyne equivalents perfectly complements the applicant’s strong background in photocatalysis and therefore guarantees two-way-transfer of knowledge between the host group and the ER (Experienced Researcher). The successful implementation of this action in the highly international and interdisciplinary environment of ICIQ and Novartis will enable the fellow to develop a unique research profile and will be crucial in building an independent academic career.
Fields of science (EuroSciVoc)
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques.
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques.
- medical and health sciencesbasic medicinepharmacology and pharmacydrug discovery
- natural scienceschemical sciencescatalysisphotocatalysis
- medical and health sciencesbasic medicinemedicinal chemistry
- medical and health sciencesbasic medicinepharmacology and pharmacypharmaceutical drugsantibiotics
- medical and health sciencesbasic medicinepharmacology and pharmacypharmaceutical drugsantivirals
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Keywords
Programme(s)
- HORIZON.1.2 - Marie Skłodowska-Curie Actions (MSCA) Main Programme
Funding Scheme
HORIZON-TMA-MSCA-PF-EF - HORIZON TMA MSCA Postdoctoral Fellowships - European FellowshipsCoordinator
43007 Tarragona
Spain