BIS-QUINOXALINECARBOXAMIDES AND BIS-NAPHTYLCARBOXAMIDES DERIVATES - SYNTHESIS, DNA INTERACTION ASSAYS AND ANTINEOPLASTIC ACTIVITY

By acylation of alpha, omega-diamines and N,N'-di-(3-aminopropyl)-pype razine, eight bis-amides derived from quinoxaline and naphthalene have been synthesized. Antineoplastic activity on human cellular lines and DNA binding of these compounds by U.V. spectroscopy were evaluated. Q uinoxalinecarboxamides showed low DNA affinity. Naphthylcarboxamides h ad no affinity at all. They were active on cellular lines in concentra tion of 10(-4)M and some of them in 10(-5)M levels. However, they disp layed high citotoxic activity, except one of them (6) which was select ed by the N.C.I. to perform in vivo screening.