Synthesis, biological activity and preliminary in silico ADMET screening of polyamine conjugates with bicyclic systems

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Abstract

Polyamine conjugates with bicyclic terminal groups including quinazoline, naphthalene, quinoline, coumarine and indole have been obtained and their cytotoxic activity against PC-3, DU-145 and MCF-7 cell lines was evaluated in vitro. Their antiproliferative potential differed markedly and depended on both their chemical structure and the type of cancer cell line. Noncovalent DNA-binding properties of the most active compounds have been examined using ds-DNA thermal melting studies and topo I activity assay. The promising biological activity, DNA intercalative binding mode and favorable drug-like properties of bis(naphthalene-2-carboxamides) make them a good lead for further development of potential anticancer drugs.

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Szumilak, M., Galdyszynska, M., Dominska, K., Bak-Sypien, I. I., Merecz-Sadowska, A., Stanczak, A., … Piastowska-Ciesielska, A. W. (2017). Synthesis, biological activity and preliminary in silico ADMET screening of polyamine conjugates with bicyclic systems. Molecules, 22(5). https://doi.org/10.3390/molecules22050794

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