Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 115, Issue -, Pages 179-190Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.03.031
Keywords
[1,5]-Naphthyridines; Topoisomerase I; Enzyme inhibition; Antiproliferative effect
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Funding
- Direccion General de Investigacion del Ministerio de Economia, Ciencia e Innovacion (MICINN, Madrid DGI) [CTQ2015-67871-R]
- Gobierno Vasco, Universidad del Pais Vasco (GV) [IT 992-16]
- Aage & Johann Louis-Hansens foundation
- Dagmar Marshalls foundation
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In an effort to establish new candidates with improved anticancer activity, we report here the synthesis of various series of 7H-indeno[2,1-c][1,5]-naphthyridines and novel 7H-indeno[2,1-c][1,5]-naphthyridine-7-ones and 7H-indeno[2,1-c][1,5]-naphthyridine-7-ols. Most of the products which were synthesized were able to inhibit Topoisomerase I activity. Moreover, in vitro testing demonstrated that a subset of the products exhibited a cytotoxic effect on cell lines derived from human breast cancer (BT 20), human lung adenocarcinoma (A 549), or human ovarian carcinoma (SKOV3). (C) 2016 Elsevier Masson SAS. All rights reserved.
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