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Content archived on 2024-06-18

THE SYNTHESIS OF DIAZOBENZOFLUORENE ANTITUMOR ANTIBIOTICS: LOMAIVITICINS A, B AND KINAMYCIN C

Objective

The proposed research describes a strategy for the convergent synthesis of diazobenzofluorene containing antitumor antibiotics Lomaiviticins A and B as well as the structurally related Kinamycin C. They are potent DNA cleaving agents and exhibit remarkable activity against a broad spectrum of cancer cell lines. These structurally novel antitumor antibiotics have a unique cytotoxicity profile, compared to other known DNA-damaging anticancer drugs such as adriamycin and mitomycin C, which may suggest a different mechanism of interaction with DNA. However, the currently limited availability of these compounds isolated by fermentation and the present lack of any methodology to generate synthetic analogs could hamper further research in the analysis of these highly potent DNA-cleaving agents. Access to these natural products as well as their analogs by means of chemical synthesis, would enable the scientific community to elucidate their mode of action and the origin of their cytotoxicity. Thus, in the absence of an alternative state of the art and given the potential of these molecules to become therapeutic cancer agents, the main objectives of the proposed project are: a) the development of a synthetic methodology for the convergent synthesis of lomaiviticins and their analogs, b) extension of this methodology towards the synthesis of the structurally related antitumor antibiotic kinamycin C, and c) the design and synthesis of structurally diverse diazobenzo[a]fluorene analogs aiming to identify new cytotoxic agents and some of the structural features required for their biological activity.

Fields of science (EuroSciVoc)

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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)

Topic(s)

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Call for proposal

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FP7-PEOPLE-2007-4-3-IRG
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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.

MC-IRG - International Re-integration Grants (IRG)

Coordinator

PANEPISTIMIO IOANNINON
EU contribution
€ 100 000,00
Address
PANEPISTEMIOYPOLE PANEPISTEMIO IOANNINON
451 10 IOANNINA
Greece

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Region
Βόρεια Ελλάδα Ήπειρος Ιωάννινα
Activity type
Higher or Secondary Education Establishments
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Total cost

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.

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