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Updated: Sep 29, 2026

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
Published on: May 28, 2014
Dialkylaminoalkylindolonaphthyridines as potential antitumour agents: synthesis, cytotoxicity and DNA binding
Lisa Dalla Via1, Ornella Gia, Sebastiano Marciani Magno
1Dipartimento di Scienze Farmaceutiche, Università di Padova, Via Marzolo 5, 35131 Padua, Italy. lisa.dallavia@unipd.it
Abstract:
The synthesis of new planar derivatives characterised by the presence of an indolonaphthyridine nucleus, carrying a dimethylaminoethyl or a dimethylaminopropyl side chain is reported. The antiproliferative activity of the new products was tested by means of an in vitro assay on human tumour cell lines (HL-60 and HeLa). A number of compounds (1a-d, 1h) showed IC(50) values comparable to that obtained with the well-known drug ellipticine on the HL-60 cell line. The interaction with DNA was also investigated. Linear flow dichroism measurements allowed us to understand the interaction geometry. The thermodynamic parameters of the binding process, i.e. intrinsic binding constant and exclusion parameter, were determined by fluorimetric titration.
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