Objective
Modern drug discovery is facing critical challenges. Rapid advances in human biology are revealing new biomolecular targets and processes, for which existing chemical compound libraries can provide only limited success in the identification of novel bioactive agents. This deficiency has been attributed primarily to the relative lack of structural diversity within the libraries. The three-dimensional world of biological macromolecules has been continuously interrogated with generally similar planar, aromatic, and structurally simple compounds. Contemporary diversity-generating methods have never been implemented for the preparation of large libraries, as an increase in the number of diverse members requires a corresponding increase in the number of synthetic steps, or a continuous supply of different staring materials. This proposal details a strategy for developing a chemically sustainable diversification method, by tapping into our largest source of organic compounds: arenes.
The proposed research aims to develop new methods that can rapidly convert simple aromatic entities into highly functionalized, complex small molecules. By integration of this strategy with many different chemical operations, numerous distinctive and independent dearomative programs will generate a diverse set of multiplex small molecules. This simplicity-to-complexity approach will provide a practical platform for the rapid, controlled access to a functionally diverse set of compounds, ranging from anticancer to anti-infective agents. This research will also deliver methods for dearomative diversification of existing aromatic compound libraries to provide new members with unique physiochemical properties. Given the broad scope of possible dearomative programs that will be developed, and the vast amount of aromatic compounds accessible, this will ultimately provide a sustainable source of diverse molecules for the next generation of compound libraries.
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. See: The European Science Vocabulary.
CORDIS classifies projects with EuroSciVoc, a multilingual taxonomy of fields of science, through a semi-automatic process based on NLP techniques. See: The European Science Vocabulary.
- medical and health sciences basic medicine pharmacology and pharmacy drug discovery
- natural sciences chemical sciences organic chemistry hydrocarbons
- natural sciences chemical sciences organic chemistry aromatic compounds
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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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H2020-EU.1.1. - EXCELLENT SCIENCE - European Research Council (ERC)
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.
ERC-STG - Starting Grant
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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) ERC-2018-STG
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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.
27100 Pavia
Italy
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.