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Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action.
Spaczynska, Ewelina; Mrozek-Wilczkiewicz, Anna; Malarz, Katarzyna; Kos, Jiri; Gonec, Tomas; Oravec, Michal; Gawecki, Robert; Bak, Andrzej; Dohanosova, Jana; Kapustikova, Iva; Liptaj, Tibor; Jampilek, Josef; Musiol, Robert.
Afiliação
  • Spaczynska E; Institute of Chemistry, University of Silesia, 75 Pulku Piechoty 1a, 41-500, Chorzów, Poland.
  • Mrozek-Wilczkiewicz A; A. Chelkowski Institute of Physics and Silesian Center for Education and Interdisciplinary Research, University of Silesia, 75 Pulku Piechoty 1a, 41-500, Chorzów, Poland.
  • Malarz K; A. Chelkowski Institute of Physics and Silesian Center for Education and Interdisciplinary Research, University of Silesia, 75 Pulku Piechoty 1a, 41-500, Chorzów, Poland.
  • Kos J; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Odbojarov 10, 832 32, Bratislava, Slovakia.
  • Gonec T; Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1, Brno, 612 42, Czech Republic.
  • Oravec M; Global Change Research Institute CAS, Belidla 986/4a, Brno, 603 00, Czech Republic.
  • Gawecki R; A. Chelkowski Institute of Physics and Silesian Center for Education and Interdisciplinary Research, University of Silesia, 75 Pulku Piechoty 1a, 41-500, Chorzów, Poland.
  • Bak A; Institute of Chemistry, University of Silesia, 75 Pulku Piechoty 1a, 41-500, Chorzów, Poland.
  • Dohanosova J; Central Laboratories, Faculty of Chemical and Food Technology, Slovak University of Technology in Bratislava, Radlinskeho 9, Bratislava, 81237, Slovakia.
  • Kapustikova I; Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Comenius University, Odbojarov 10, 832 32, Bratislava, Slovakia.
  • Liptaj T; Central Laboratories, Faculty of Chemical and Food Technology, Slovak University of Technology in Bratislava, Radlinskeho 9, Bratislava, 81237, Slovakia.
  • Jampilek J; Department of Analytical Chemistry, Faculty of Natural Sciences, Comenius University, Ilkovicova 6, 842 15, Bratislava, Slovakia. josef.jampilek@gmail.com.
  • Musiol R; Regional Centre of Advanced Technologies and Materials, Faculty of Science, Palacky University, Slechtitelu 27, 783 71, Olomouc, Czech Republic. josef.jampilek@gmail.com.
Sci Rep ; 9(1): 6387, 2019 04 23.
Article em En | MEDLINE | ID: mdl-31011161
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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Proteína Supressora de Tumor p53 / Naftóis / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Desenho de Fármacos / Proteína Supressora de Tumor p53 / Naftóis / Antineoplásicos Limite: Humans Idioma: En Ano de publicação: 2019 Tipo de documento: Article