Objective
Research objectives and content
Since early work established between vitamin D3 and rickets, the importance has emerged of vitamin D3 and the hormonally active form, la,25-dihidroxyvitamin D3 1 in a number of disease funtions. recent research suggests that 1 has potential as a treatment for psoriasis, and for certain cancers. effective chemotherapy must combine lo hypercalcemic action with high anti-cancer activity and the search has begun for analogues which meet these criteria.
We propose to develop a general synthetic strategy for the assembly of analogues of 1. The strategy has been devised so as to combine optimal convergence, brevity and stereoselectivity in such a way that it will be possible to synthetize a structurally diverse range of vitamine D3 analogues hitherti inaccesible using established semi-synthetic or degradation based methods. The key disconnections are shown in Scheme. It is proposed to established the intermediancy of 'southern hemisphere' and 'northern hemisphere' fragment 3 and 4, which will be joined using transition metalmediated coupling reactions to give structures exmplified by triene 2. The functionality necesary for the connecting of 3 and 4 in this way will be incorporate directly from the strategy-level transformations used in their synthesis, requiring only minimal manipulation of the products of these reactions immediately prior to the crucial coupling reaction. attachment to C-22 of a variety of nuclephilic side-chain units will be accomplished using established methods of olefination and alkylation.
Training content (objective, benefit and expected impact)
This project will be very useful to the training of the candidate because I should develop synthetic methods which are important for our research group in Spain. Secondly, I will be working in Medicinal Chemistry that is the main object I would like work in my future research programme. Finally, I will have the opportunity of using materials and instruments that I did not use in my Ph.D. studies. We believe that once we have established the scope for the elaboration of (1), many related biologically important analogues will ill succumb to total synthesis via a similar strategy.
Links with industry / industrial relevance (22)
Professor Craig has received several medals and Awards from the Cheical Industry for his research accomplishmentes, and consults widely for the Chemical Industry on several aspect of organic synthesis. In the same time, and following one of the EC 's guidelines, the project would enanble the the transfer of information a positive results toward the european Pharmaceutical Industry.
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 medicinal chemistry
- medical and health sciences clinical medicine oncology
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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.
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.
Call for proposal
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Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.
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.
Coordinator
SW7 2AZ LONDON
United Kingdom
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.