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Abstract

The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino; R.sup.2 is hydrogen, hydroxy, methoxy or amino; R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy; R.sup.4 is hydrogen, hydroxy or amino; Z is --CH.sub.2 --, --O-- or --NH--; and a) X.sup.1 is hydrogen; X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; and X.sup.3 is hydrogen or hydroxy; or b) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogen or a pharmaceutically acceptable salt thereof provided that: i) at least one of R.sup.1 through R.sup.4 is other than hydrogen; ii) when R.sup.1 is methoxy, R.sup.2 is hydroxy or methoxy, R.sup.3 is hydrogen or methoxy and R.sup.4 is hydrogen; iii) when R.sup.2 is hydroxy, methoxy or amino, R.sup.3 is hydrogen, hydroxy or methoxy, and R.sup.4 is hydrogen; iv) when R.sup.4 is hydroxy or amino, R.sup.1 and R.sup.3 are hydrogen and R.sup.2 is hydroxy or amino; and. v) when R.sup.1 is fluoro, chloro, iodo or amino, R.sup.2 is hydrogen, hydroxy or methoxy, R.sup.3 is hydrogen, hydroxy or methoxy and R.sup.4 is hydrogen and the use of these compounds as topoisomerase inhibitors and antitumor agents.

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First Claim