Ricerc@Sapienza

Cancer worldwide remains one of the most important cause of death. Tumors that recur after an initial response to chemotherapy easily become resistant to multiple drugs, making more difficult the cancer treatment. The present research project aims to design and synthesize new anticancer drugs targeting tubulin. Arylthioindoles and aroylindoles are a modern class of tubulin polymerization inhibitors that proved effective in inhibiting many cancer cells lines. Derivatives bearing a cyclic substituent at the position 2 of the indole inhibit tubulin assembly by binding the colchicine site of tubulin at submicromolar concentration and cell growth at low nanomolar concentrations. In this research project, will be carried out exhaustive structure activity relationship studies mainly focusing on positions 6-7 of the indole nucleus by introducing an aromatic or heteroaromatic ring to identify new potent tubulin polymerization inhibitors.