Ricerc@Sapienza

3-Aroyl-1,4-diarylpyrroles (ARDAPs) are potent inhibitors of tubulin polymerization and cancer cell growth by binding the colchicine site of tubulin, recently developed by our research group. Preliminary results suggested that the introduction of a heterocycle at position 4 of the pyrrole ring, and the simultaneous presence of a 3-aminophenyl group at position 1 increase both tubulin polymerization and anticancer activity. However, the new compounds, such as colchicine, showed a low solubility in water. Starting from these data, this research project aims to optimise the pharmacokinetic profile of ARDAP derivates. In particular, we will try to improve the water solubility by introducing linear chains, bearing various combinations of amino acids residues, on the amino group on the 3-aminophenyl group at position 1 of the pyrrole nucleus.