Project Overview

Lipids are central to the regulation and control of cellular function and to disease, and lipidomics is beginning to make signifi­cant contri­butions to our understanding of cellular and pathophysiological processes. Alkyllysophospholipid analogues have recently received much attention due to their antineoplastic, immunomodulatory and antiparasitic properties. ''Sopholides'' aims at developing cost effective, reliable and efficient technologies based on solid phase chemistry (SPOS) for the synthesis of ether phospholipid analogues. Focused libraries will be synthesized with the aim of optimization of structural features of lead compounds produced at the laboratories of the Institute of Biology, Medicinal Chemistry and Biotechnology, Division of Organic & Medicinal Chemistry (OMC) for specific biological applications including antiprotozoal therapeutics and anticancer compounds. In parallel, SPOS will be used to prepare dendrimeric materials and, in particular, dendrimer-modified resins designed to provide increased loading capacity for solid supports. These modified resins will be evaluated for phospholipid solid phase synthesis. To comple­ment these activities, the use of High-Energy Techniques with microwaves and ultrasound, whose special applicability to SPOS is well-documented, will also be investigated.

''Sopholides'' is being made jointly by members of the Pharmaceutical Chemistry (PCG) (Dr T. Calogeropoulou) and the Organic and Organometallic Chemistry Group (OMG) (Dr M. Micha-Screttas, Dr B. Steele, Dr G. Heropoulos).

By hosting experienced researchers as well as by interacting with the multidisciplinary expertise of the 3 Partner groups (Prof Mark Bradley, University of Edinburgh, Prof. Tim Mason, Coventry University, Dr Andre Loupy, Universite Paris-Sud), this project aims for the transfer of knowledge in these key areas and techniques in order to maintain the momentum of the research of the Host Institute and to improve its competitiveness at national and international level , not only in medicinal chemistry but also in its other activities such as the generation of ligands for homogeneous catalysis and of functional organic materials.

The specific knowledge and advanced skills, which will be developed through the course of the ToK project, will benefit both basic research and the potential industrial applications. Furthermore, this approach in not applied by other pharmaceutical chemistry departments in Greece.