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

J 2019

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

SPACZYNSKA, E, A MROZEK-WILCZKIEWICZ, K MALARZ, J KOS, Tomáš GONĚC et. al.

Základní údaje

Originální název

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

Autoři

SPACZYNSKA, E, A MROZEK-WILCZKIEWICZ, K MALARZ, J KOS, Tomáš GONĚC, M ORAVEC, R GAWECKI, A BAK, J DOHANOSOVA, I KAPUSTIKOVA, T LIPTAJ, J JAMPILEK a R MUSIOL

Vydání

Nature Scientific Reports, London, NATURE PUBLISHING GROUP, 2019, 2045-2322

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Utajení

není předmětem státního či obchodního tajemství

Impakt faktor

Impact factor: 3.998

DOI

http://dx.doi.org/10.1038/s41598-019-42595-y

UT WoS

000465214900004

Příznaky

Mezinárodní význam, Recenzováno

Změněno: 9. 3. 2021 23:38, PharmDr. Tomáš Goněc, Ph.D.

Anotace

V originále

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.

Citovat

SPACZYNSKA, E, A MROZEK-WILCZKIEWICZ, K MALARZ, J KOS, Tomáš GONĚC, M ORAVEC, R GAWECKI, A BAK, J DOHANOSOVA, I KAPUSTIKOVA, T LIPTAJ, J JAMPILEK a R MUSIOL. Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action. Nature Scientific Reports. London: NATURE PUBLISHING GROUP, 2019, roč. 9, 16 s. ISSN 2045-2322. Dostupné z: https://dx.doi.org/10.1038/s41598-019-42595-y.

@article{1727056,
   author = {Spaczynska, E and MrozekandWilczkiewicz, A and Malarz, K and Kos, J and Goněc, Tomáš and Oravec, M and Gawecki, R and Bak, A and Dohanosova, J and Kapustikova, I and Liptaj, T and Jampilek, J and Musiol, R},
   article_location = {London},
   doi = {http://dx.doi.org/10.1038/s41598-019-42595-y},
   language = {eng},
   issn = {2045-2322},
   journal = {Nature Scientific Reports},
   title = {Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action},
   volume = {9},
   year = {2019}
}

TY  - JOUR
ID  - 1727056
AU  - Spaczynska, E - Mrozek-Wilczkiewicz, A - Malarz, K - Kos, J - Goněc, Tomáš - Oravec, M - Gawecki, R - Bak, A - Dohanosova, J - Kapustikova, I - Liptaj, T - Jampilek, J - Musiol, R
PY  - 2019
TI  - Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action
JF  - Nature Scientific Reports
VL  - 9
PB  - NATURE PUBLISHING GROUP
SN  - 20452322
N2  - 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.
ER  -

SPACZYNSKA, E, A MROZEK-WILCZKIEWICZ, K MALARZ, J KOS, Tomáš GONĚC, M ORAVEC, R GAWECKI, A BAK, J DOHANOSOVA, I KAPUSTIKOVA, T LIPTAJ, J JAMPILEK a R MUSIOL. Design and synthesis of anticancer 1-hydroxynaphthalene-2-carboxanilides with a p53 independent mechanism of action. \textit{Nature Scientific Reports}. London: NATURE PUBLISHING GROUP, 2019, roč.~9, 16 s. ISSN~2045-2322. Dostupné z: https://dx.doi.org/10.1038/s41598-019-42595-y.

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