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A series of 7-nitro- and amino-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. There of the 7-nitro derivatives (12, 14, and 15) were found to have 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%). 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. Tm data suggest that these compounds bind to DNA and are strong inhibitors of the polymerase reaction (I50 = 6-9 X 10(-6) M).
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
November 1989,
Chemical & pharmaceutical bulletin,
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
August 2008,
Journal of medicinal chemistry,
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
November 2005,
Medicinal chemistry (Shariqah (United Arab Emirates)),
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
March 1949,
Journal of the American Chemical Society,
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
August 1985,
Journal of medicinal chemistry,
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
June 2009,
Molecules (Basel, Switzerland),
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
May 2010,
Bioorganic & medicinal chemistry,
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
January 2020,
Bioorganic & medicinal chemistry letters,
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
December 1965,
Zeitschrift fur Haut- und Geschlechtskrankheiten,
B K Sinha, and
R M Philen, and
R Sato, and
R L Cysyk
March 2007,
European journal of medicinal chemistry,
