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Title: Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action
Authors: Spaczyńska, Ewelina
Mrozek-Wilczkiewicz, Anna
Malarz, Katarzyna
Kos, Jiri
Gonec, Tomas
Orave, Michal
Gawecki, Robert
Bąk, Andrzej
Musioł, Robert
Dohanosova, Jana
Kapustikova, Iva
Liptaj, Tibor
Jampilek, Josef
Keywords: 1-hydroxynaphthalene-2-carboxanilides; Design and synthesis; anticancer
Issue Date: 2019
Citation: Scientific Reports, Vol. 9 (2019), Art. No. 6387
Abstract: A series of 116 small-molecule 1-hydroxynaphthalene-2-carboxanilides was designed based on the fragment-based approach and was synthesized according to the microwave-assisted protocol. The biological activity of all of the compounds was tested on human colon carcinoma cell lines including a deleted TP53 tumor suppressor gene. The mechanism of activity was studied according to the p53 status in the cell. Several compounds revealed a good to excellent activity that was similar to or better than the standard anticancer drugs. Some of these appeared to be more active against the p53 null cells than their wild-type counterparts. Intercalating the properties of these compounds could be responsible for their mechanism of action.
DOI: 10.1038/s41598-019-42595-y
ISSN: 2045-2322
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