Synthesis and antitumor properties of bis (quinaldine) derivatives

Article abstract of DOI:10.1021/jm00221a037

A series of 7-nitro. and amino-N,N'-bis(4-quinaldinyl)-αω-diaminoalkanes related to the 6-amino derivative was synthezied and tested in the mouse P-388 lymphocytic leukemia screen. Three of the 7-nitro derivatives were found to have moderate activity (T/C 140-150%), while other nitro derivatives were devoid of any antitumor properties. All five 7-amino compounds were moderately to strongly active (T/C 134-196%). In addition, binding of amino derivatives 2-6 to DNA was examined by their ability to (1) stabilize DNA to thermal denaturation and (2) inhibit the DNA-dependent RNA polymerase reaction in vitro. T(m) data suggest that these compounds bind to DNA and are strong inhibitors of the polymerase reaction (I₅₀ = 6-9 X 10^-6 M).