A series of indolo[3,2-c]cinnoline derivatives was prepared and tested to e
valuate their biological activity. Most of them inhibited the proliferation
of leukemia, lymphoma and solid tumor-derived cell lines at micromolar con
centrations, whereas none of the compounds were active against HIV-1. With
the exception of 7g, all title compounds showed antibacterial activity agai
nst grampositive bacteria, being up to 200 times more potent than the refer
ence drug streptomycin. Some of the indolo[3,2-c]cinnolines were also endow
ed with good antifungal activity, particularly against Cryptococcus neoform
ans. (C) 1999 Elsevier Science Ltd. All rights reserved.