Design and Synthesis of Anticancer 1-Hydroxynaphthalene-2-carboxanilides with p53 Independent Mechanism of Action

0504156 - ÚVGZ 2020 RIV GB eng J - Journal Article
Spaczynska, E. - Mrozek-Wilczkiewicz, A. - Malarz, K. - Kos, J. - Goněc, T. - Oravec, Michal - Gawecki, R. - Bak, A. - Doháňošová, J. - Kapustíková, I. - Liptaj, T. - Jampílek, J. - Musiol, R.
Design and Synthesis of Anticancer 1-Hydroxynaphthalene-2-carboxanilides with p53 Independent Mechanism of Action.
Scientific Reports. Roč. 9, apr (2019), č. článku 6387. ISSN 2045-2322. E-ISSN 2045-2322
R&D Projects: GA MŠMT(CZ) EF16_013/0001609; GA MŠMT(CZ) LO1415
Research Infrastructure: CzeCOS II - 90061
Institutional support: RVO:86652079
Keywords : Microwave-assisted synthesis * cancer-cell-lines * subtituted salicylanilides * enzalutamide resistance * acquired-resistance * herbicidal activity * biological-activity * in-vitro * apoptosis * dna
OECD category: Oncology
Impact factor: 3.998, year: 2019
Method of publishing: Open access
https://www.nature.com/articles/s41598-019-42595-y

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.
Permanent Link: http://hdl.handle.net/11104/0295851