Synthesis, cytotoxic evaluation, and DNA binding of novel thiazolo[5,4-b]quinoline derivatives

A series of novel alkylamino and 9-anilinothiazolo[5,4-b]quinolines were synthesized as potential antitumoral agents. The in vitro cytotoxicity of these compounds was evaluated on several cell lines. The inclusion of electron-withdrawn/acceptor hydrogen-bond groups at position 3′ of the anilino ring and the presence of an alkylamino chain on the tricyclic framework (regardless of its position) seem to be structural features relevant to cytotoxic activity.

Electron-withdrawing/electron-releasing substituents attached at 3′ and 4′-position of anilino ring or alkylamino residues were relevant to the cytotoxicity and DNA intercalation of several novel thiazolo[5,4-b]quinoline derivatives.Figure optionsDownload as PowerPoint slide