Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 87, Issue -, Pages 805-813Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.10.015
Keywords
Oxadiazolines; Naphthalene; Synthesis; Anticancer activity; Drug-likeness; In silico toxicity
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Funding
- BIPPED2 [S2010/BMD-2457]
- Comunidad de Madrid
- MINECO [BIO2013-42984-R]
- Magnus Ehrnrooth Foundation [ME2012n44]
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A series of new oxadiazoline-substituted naphthalenyl acetates 3a-e and oxadiazoline-substituted 4-methoxynaphthalenyl acetates 7b-e were synthesized and tested by the National Cancer Institute (NCI) for their in vitro anticancer activity. The two derivatives bearing acetoxy groups at the 1 and 3 positions of the phenyl ring 3c and 7c were the most active showing significant anticancer activity against all tested cancer cell lines, with GI(50) values ranging from 0.175 to 3.91 mu M, and 0.306-11.7 mu M, respectively. The selectivity of compound 3c was greater for non-solid tumor cell lines. Computational prediction of molecular and pharmacokinetic properties revealed that both compounds are safe and compound 7c had a good drug-likeness score. (c) 2014 Elsevier Masson SAS. All rights reserved.
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