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With the aim of obtaining new bifunctional intercalators for DNA, a new series of bis-pyridoquinolines were synthesized by joining two tricyclic planar moieties through a flexible chain. For preparing the corresponding potential monofunctional intercalators also a series of mono-pyridoquinolines were prepared by chemical synthesis by joining the same chromophore with a flexible side-chain. The melting profiles of the complexes between two bis-pyridoquinolines and DNA showed two different thermal transitions supporting the bis-intercalation of the ligand with the macromolecule. On the other hand, two mono-pyridoquinolines showed only one transition in the melting profile indicating a behaviour consistent with a mono-intercalation. The antiproliferative activity was tested in terms of DNA synthesis inhibition in Ehrlich ascite tumor cells; the examined bis-intercalating agent showed to be much more active than the tested mono-intercalating compound.
G Malesani, and
G Chiarelotto, and
M G Ferlin, and
F Bordin, and
F Baccichetti, and
F Carlassare, and
D Vedaldi, and
F Dall'Acqua
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Biochemical pharmacology,
G Malesani, and
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F Carlassare, and
D Vedaldi, and
F Dall'Acqua
August 2013,
International journal of molecular sciences,
G Malesani, and
G Chiarelotto, and
M G Ferlin, and
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D Vedaldi, and
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May 2011,
Accounts of chemical research,
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M G Ferlin, and
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October 2022,
Chemical biology & drug design,
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January 1986,
Basic life sciences,
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F Dall'Acqua
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Drugs under experimental and clinical research,
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F Dall'Acqua
February 1982,
Biochemical and biophysical research communications,
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G Malesani, and
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Journal of the American Chemical Society,
