6,9-Bis((aminoalkyl)amino)benzo(g)isoquinoline-5,10-diones.A Novel Class of Chromophore-Modified Antitumor Anthracene-9,10diones: Synthesis and Antitumor Evaluations.-In a search for analogues with optimal therapeutic efficacy, a series of aza analogues of (I) is prepared by reaction of (V) with the appropriate amines in a similar manner as described for (IIa) (isolated as hydrochloride). Mitoxantrone (I) is a known antitumor agent, accompanied by toxic side effects. Compounds (IIb) and (IIc) show in vitro activities against L1210 murine leukemia similar to (I), but all aza analogues have decreased cytotoxic potency in both the sensitive and the doxorubicin-resistant LoVo human colon adenocarcinoma cell line compared with (I). In vivo antitumor activity against P388 murine leukemia of (IIb) and (IId) is comparable and of (IIa) superior to that of (I). Therefore (IIa), which is not cardiotoxic and less leukopenic than (I), appears to be the most promising aza analogue for further clinical evaluation. -(KRAPCHO, A. P.; PETRY, M. E.; GETAHUN, Z.; LANDI, J. J. JUN.; STALLMAN, J.; POLSENBERG, J. F.; GALLAGHER, C. E.; MARESCH, M. J.; HACKER, M. P.; GIULIANI, F. C.; BEGGIOLIN, G.; PEZZONI, G.; MENTA, E.; MANZOTTI, C.; OLIVA, A.; SPINELLI, S.; TOGNELLA, S.; J. Med. Chem. 37 (1994) 6, 828-837; Dep.
