K. Gorlitzer et al., ANTI-MALARIA ACTIVE 10H-INDOL[3,2-B]QUINO LINE-11-YLAMINES .1. PHENOL-MANNICH-BASES OF THE AMODIAQUINE AND CYCLOQUINE TYPE, Die Pharmazie, 49(4), 1994, pp. 231-235
The 11-chloro-quindoline derivatives 3 react with 4-aminophenol and th
e mono- and bis-phenol-Mannich-bases 6 to yield the 10 H-indolo[3,2-b]
quinoline-11-yl-amines 4 and 7. The amodiaquine analogue 7a as the bes
t of all compounds shows a comparable activity with choroquine and inh
ibits a multiresistant Plasmodium falciparum strain at the same concen
tration. Compound 7e from the cycloquine-type was selected for an in v
ivo antitumor screening programme.