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Synthesis and biological evaluation of indeno[1,5]naphthyridines as topoisomerase I (TopI) inhibitors with antiproliferative activity.

Authors :
Alonso, Concepción
Fuertes, María
González, María
Rubiales, Gloria
Tesauro, Cinzia
Knudsen, Birgitta R.
Palacios, Francisco
Source :
European Journal of Medicinal Chemistry. Jun2016, Vol. 115, p179-190. 12p.
Publication Year :
2016

Abstract

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). [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
115
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
114524693
Full Text :
https://doi.org/10.1016/j.ejmech.2016.03.031