Bis-pyridoquinolines as new bifunctional intercalators for DNA.
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.
D000634:Aminoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D002417:Cattle; D055598:Chemical Phenomena; D002621:Chemistry; D003432:Cross-Linking Reagents / Q000138:chemical synthesis*; D004247:DNA / Q000032:analysis*; D066298:In Vitro Techniques; D007364:Intercalating Agents / Q000138:chemical synthesis*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology
D000634:Aminoquinolines; D003432:Cross-Linking Reagents; D007364:Intercalating Agents; D011725:Pyridines; D004247:DNA