Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 62, Issue -, Pages 130-138Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.12.039
Keywords
Oxo-heterocyclic; Naphthalimides; Antitumor agents; Topo I; Topo II; DNA intercalation
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Funding
- National Basic Research Program of China (973 Program) [2010CB126100]
- National High Technology Research and Development Program of China (863 Program) [2011AA10A207]
- China 111 Project [B07023]
- Fundamental Research Funds for the Central Universities
- Shanghai Committee of Science and Technology [11DZ2260600]
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Three series of novel oxo-heterocyclic fused naphthalimide derivatives (8a-8f, 13a-13d, 17a-17d) were prepared. The newly-synthesized compounds, and their thio-heterocyclic fused analogs (1a-1c, 2a-2d, 3a-3c) exhibited potent antiproliferative activity correlated well with their structure. Further research demonstrated that all the representative compounds 13a, 2a and 17a, 3a showed strong inhibition activity to topo II similarly with amonafide, and also potent topo I inhibition activity, which was seldom reported before for naphthalimide derivatives. Preliminary exploration proved their DNA sequence preference. In all, dual topo I/topo II inhibition and DNA sequence preference might contribute to enhancing tumor selectivity and overcoming drug resistance. (C) 2013 Elsevier Masson SAS. All rights reserved.
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