A series of 7-nitro- and amino-N,N''-bis(4-quinaldinyl)-.alpha.,.omega.-diaminoalkanes related to the 6-amino derivative 1 was synthesized and tested in the mouse P-388 lymphocytic leukemia screen. Three of the 7-nitro derivatives (12, 14 and 15) had moderate activity (T/C 140-150%), while other nitro derivatives (11 and 13) were devoid of any antitumor properties. All five 7-amino compounds (2-6) were moderately to strongly active (T/C 134-196%). Binding of amino derivatives 2-6 to DNA was examined by their ability to stabilize DNA to thermal denaturation and inhibit the DNA-dependent RNA polymerase reaction in vitro. Tm [melting temperature] data suggest that these compounds bind to DNA and are strong inhibitors of the polymerase reaction (I50 = 6-9 .times. 1006 M).