Objective
This proposal falls into the area of construction of diversity-oriented natural product-like libraries for chemical biology and drug discovery purposes. The synthesis of such libraries requires the availability of efficient and practical methods, including asymmetric transformations with high degree of stereoselectivity, for the multistep solid-phase synthesis of frameworks of biologically promising natural products. The objectives are:1) Solid-phase synthesis of 5- and 6-membered ring lactones (compounds c losely related to some biologically active natural products),2) solid-phase synthesis of a Cytostatin-derived compound library. Cytostatin is a natural product isolated from a Streptomyces strain that inhibits the serine/threonine phosphatase 2A at submicr omolar concentration,3) biological evaluation of the compound libraries in biochemical screens (in vitro inhibition assays) by me in close collaboration with specialised scientists in the field.Targets 1 and 2 will be achieved by means of an enantioselecti ve allylation or crotylation reaction of chiral polymer-supported aldehydes as the key step (which has no precedents to the date, only previous studies in Waldmann group but still unpublished), followed by a lactonization process. This presumably will lead to a library of 5- and 6-membered ring lactones with a side chain in the ring. The points of generation of molecular diversity will be: modification in the size and variation in the substitution pattern of the lactone ring. Concerning the side chain, it w ill be modified mainly by using the alkene reactivity.The main aim is to increase the knowledge and interest of the scientific community in the use of asymmetric strategies in solid-phase synthesis and drug discovery. In addition, I expect to acquire new s kills and expertise in chemical biology to complement my research background.
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 aldehydes
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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.
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
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.
FP6-2004-MOBILITY-5
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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
DORTMUND
Germany
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.