A series of bis-intercalators bearing the 1,8-naphthalimide chromophor
e has been synthesized and in vitro activities determined. Most compou
nds have higher activities in HT-29 than the leader compounds Mitonafi
de and Amonafide. One of them (22) was selected for in vivo studies an
d presents an interesting activity in MX-1 and OVCAR models. (22) also
acts as antitopoisomerase II.