ChemInform Abstract: Novel Isoxazole Polycyclic Aromatic Hydrocarbons as DNA‐Intercalating Agents.

Abstract

Novel Isoxazole Polycyclic Aromatic Hydrocarbons as DNA-Intercalating Agents.-The third generation of isoxazole polycyclic aromatic hydrocarbons, possessing binding constants enabling easy diffusion of targeting remotely implanted tumors, is synthesized accordingly to the 1,3-dipolar cycloaddition methodology. The utility of this skeleton in the synthesis of structures, designed to capitalize on its intercalative properties, is investigated. In the series isoxazole-, isoxazolinyl-, isoxazolidinyl-polycyclic aromatic hydrocarbons, the latter compounds display the best intercalative properties. Especially compound (IX) exhibits good activity against all tested cell lines and particularly against human lung cancer cells. -(RESCIFINA*, A.; VARRICA, M. G.; CARNOVALE, C.; ROMEO, G.; CHIACCHIO, U.; Eur. J. Med. Chem. 51 (2012) 163-173, http://dx.