We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Synthesis and biological evaluation of new derivatives of tricyclic heteroaromatic carboxamides as potential topoisomerase I inhibitors.
- Authors
Kostina, V. G.; Alexeeva, I. V.; Lysenko, N. A.; Negrutska, V. V.; Dubey, I. Ya.
- Abstract
A series of new N-functionalized amide derivatives of phenazine-1-and acridone-4-carboxylic acids were synthesized and tested in vitro as potential topoisomerase I inhibitors. Their tricyclic heteroaromatic cores with intercalative properties contained carboxamide functions modified with pyridyl and N,N-dimethylamino groups attached via short linkers. These basic substituents are able to be protonated in water and thus could provide additional binding interactions of ligands with DNA and/or topoisomerase complex enhancing the inhibitory activity of compounds. Pyridyl-modified derivatives of both heterocycles were found to inhibit topoisomerase in vitro at 100 μM concentration, in contrast to non-modified carboxamides which are inactive against the enzyme.
- Subjects
DNA topoisomerase inhibitors; CARBOXAMIDES; AROMATIC compounds; PYRIDYL compounds; PHENAZINE
- Publication
Ukrainica Bioorganica Acta, 2016, Vol 14, Issue 1, p3
- ISSN
1814-9758
- Publication type
Article