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

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.

SUBMITTER: Spaczynska E

PROVIDER: S-EPMC6476888 | biostudies-literature | 2019 Apr

REPOSITORIES: biostudies-literature

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

Spaczyńska Ewelina E Mrozek-Wilczkiewicz Anna A Malarz Katarzyna K Kos Jiri J Gonec Tomas T Oravec Michal M Gawecki Robert R Bak Andrzej A Dohanosova Jana J Kapustikova Iva I Liptaj Tibor T Jampilek Josef J Musiol Robert R

Scientific reports 20190423 1

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 th ...[more]

PMID: 31011161

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