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Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action

E. Spaczyńska, A. Mrozek-Wilczkiewicz, K. Malarz, J. Kos, T. Gonec, M. Oravec, R. Gawecki, A. Bak, J. Dohanosova, I. Kapustikova, T. Liptaj, J. Jampilek, R. Musiol,

. 2019 ; 9 (1) : 6387. [pub] 20190423

Language English Country Great Britain

Document type Journal Article, Research Support, Non-U.S. Gov't

Persistent link   https://www.medvik.cz/link/bmc20028916

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.

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$a A series of 116 small-molecule 1-hydroxynaphthalene-2-carboxanilides was designed based on the fragment-based approach and was synthesized according to the microwave-assisted protocol. The biological activity of all of the compounds was tested on human colon carcinoma cell lines including a deleted TP53 tumor suppressor gene. The mechanism of activity was studied according to the p53 status in the cell. Several compounds revealed a good to excellent activity that was similar to or better than the standard anticancer drugs. Some of these appeared to be more active against the p53 null cells than their wild-type counterparts. Intercalating the properties of these compounds could be responsible for their mechanism of action.
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$a Mrozek-Wilczkiewicz, Anna $u A. Chełkowski Institute of Physics and Silesian Center for Education and Interdisciplinary Research, University of Silesia, 75 Pułku Piechoty 1a, 41-500, Chorzów, Poland.
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$a Malarz, Katarzyna $u A. Chełkowski Institute of Physics and Silesian Center for Education and Interdisciplinary Research, University of Silesia, 75 Pułku Piechoty 1a, 41-500, Chorzów, Poland.
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$a Kos, Jiri $u Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Odbojarov 10, 832 32, Bratislava, Slovakia.
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$a Gonec, Tomas $u Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1, Brno, 612 42, Czech Republic.
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$a Oravec, Michal $u Global Change Research Institute CAS, Belidla 986/4a, Brno, 603 00, Czech Republic.
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$a Gawecki, Robert $u A. Chełkowski Institute of Physics and Silesian Center for Education and Interdisciplinary Research, University of Silesia, 75 Pułku Piechoty 1a, 41-500, Chorzów, Poland.
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$a Bak, Andrzej $u Institute of Chemistry, University of Silesia, 75 Pułku Piechoty 1a, 41-500, Chorzów, Poland.
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$a Dohanosova, Jana $u Central Laboratories, Faculty of Chemical and Food Technology, Slovak University of Technology in Bratislava, Radlinskeho 9, Bratislava, 81237, Slovakia.
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$a Kapustikova, Iva $u Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Odbojarov 10, 832 32, Bratislava, Slovakia.
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$a Liptaj, Tibor $u Central Laboratories, Faculty of Chemical and Food Technology, Slovak University of Technology in Bratislava, Radlinskeho 9, Bratislava, 81237, Slovakia.
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$a Jampilek, Josef $u Department of Analytical Chemistry, Faculty of Natural Sciences, Comenius University, Ilkovicova 6, 842 15, Bratislava, Slovakia. josef.jampilek@gmail.com. Regional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Slechtitelu 27, 783 71, Olomouc, Czech Republic. josef.jampilek@gmail.com.
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$a Musiol, Robert $u Institute of Chemistry, University of Silesia, 75 Pułku Piechoty 1a, 41-500, Chorzów, Poland. robert.musiol@us.edu.pl.
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