Natural Products and Chemical Synthesis for the Generation of New Biologically Active Compounds

We are involved in the synthesis of new compounds potentially able to inhibit different biological targets in the frame of the exploration of the chemical space looking for any small molecule effective against cancer and angiogenesis. In particular we are considering as biological targets tubulin, topoisomerase, histone deacetylases, p53 and several tyrosine kinases. We are following two different approaches: natural products as building blocks and molecular modelling. We use natural products for the preparation of structurally simplified analogues, bivalent compounds and releasable conjugates. The use of molecular modelling (collaborative projects) guide the design of new compounds on the base of the three-dimensional structures of the biological targets with particular attention of different tyrosine kinases such as Met, VEGF and Abl.