Antitumor properties of tetrahydrobenz(a)anthraquinone derivatives

Abstract
The compound 8,11-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-6-methoxy-1,2,3,4-tetrahydro-7,12-benz[a]-anthraquinone (7) was synthesized from 3,6-dimethoxyphthalic anhydride and 6-methoxy-1,2,3,4-tetrahydronaphthalene by a Friedel-Crafts reaction, cyclization to form a dihydroxyanthraquinone, and conversion into the amino-substituted derivative by reaction with 2-[(2-hydroxyethyl)amino]ethylamine. The new compound, a ring D analogue of mitoxantrone, showed grwoth inhibition at micromolar concentrations, of murine leukemia 1210, human lung H125, human breast MCF7, human ovary 121, and human colon WiDr and increased the left span of leukemic mice by 38%.