Objective
Bioactive macrocyclic compounds are valuable platforms in drug discovery. More often than not, natural products represent attractive leads, the structures of which may be altered by chemical synthesis to enhance efficacy, lower toxicity, and superior physicochemical properties. The proposed project aims to a practical and programmable strategy for precise skeletal editing of large ring structures by aligning catalytic ring-opening metathesis, site- and/or stereoselective modification of the linear intermediates, and formation re-formation of the macrocycle through catalytic ring-closing metathesis. The advance will significantly enhance our ability to navigate hitherto unexplored chemical space, needed for drugs discovery.
The proposed investigations are centered on epothilone C, an important naturally occurring compound. We will to demonstrate the versatility of our approach by precise framework editing of this anticancer agent in a systematic way. The first phase will entail Z-to-E isomerization of the macrocyclic alkene, an alteration that will significantly change the molecule’s three-dimensional shape. This will be followed by site specific insertion of a methylene or a hydroxy methylene at one or both sides of the acyclic allylic sites. We will then re-close the ring. Similarly, ring contraction will be implemented through deletion of one or two methylene groups. Finally, ring expansion and ring contraction will be combined to achieve ring distortion.
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Keywords
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Project’s keywords as indicated by the project coordinator. Not to be confused with the EuroSciVoc taxonomy (Fields of science)
Programme(s)
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
Multi-annual funding programmes that define the EU’s priorities for research and innovation.
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HORIZON.1.2 - Marie Skłodowska-Curie Actions (MSCA)
MAIN PROGRAMME
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Topic(s)
Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.
Funding Scheme
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
Funding scheme (or “Type of Action”) inside a programme with common features. It specifies: the scope of what is funded; the reimbursement rate; specific evaluation criteria to qualify for funding; and the use of simplified forms of costs like lump sums.
HORIZON-TMA-MSCA-PF-EF - HORIZON TMA MSCA Postdoctoral Fellowships - European Fellowships
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Call for proposal
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
(opens in new window) HORIZON-MSCA-2021-PF-01
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Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.
67081 Strasbourg
France
The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.