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ATP-competitive inhibitors of human DNA topoisomerase IIα with improved antiproliferative activity based on N-phenylpyrrolamide scaffold
ID
Skok, Žiga
(
Author
),
ID
Durcik, Martina
(
Author
),
ID
Zajec, Živa
(
Author
),
ID
Gramec, Darja
(
Author
),
ID
Bozovičar, Krištof
(
Author
),
ID
Pišlar, Anja
(
Author
),
ID
Tomašič, Tihomir
(
Author
),
ID
Zega, Anamarija
(
Author
),
ID
Peterlin-Mašič, Lucija
(
Author
),
ID
Kikelj, Danijel
(
Author
),
ID
Zidar, Nace
(
Author
),
ID
Ilaš, Janez
(
Author
)
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MD5: 90814CBB076E27245E9784A10AB17FB7
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https://www.sciencedirect.com/science/article/pii/S0223523423000314
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Abstract
ATP-competitive inhibitors of human DNA topoisomerase II show potential for becoming the successors of topoisomerase II poisons, the clinically successful anticancer drugs. Based on our recent screening hits, we designed, synthesized and biologically evaluated new, improved series of N-phenylpyrrolamide DNA topoisomerase II inhibitors. Six structural classes were prepared to systematically explore the chemical space of N-phenylpyrrolamide based inhibitors. The most potent inhibitor, 47d, had an IC$_{50}$ value of 0.67 μM against DNA topoisomerase IIα. Compound 53b showed exceptional activity on cancer cell lines with IC$_{50}$ values of 130 nM against HepG2 and 140 nM against MCF-7 cancer cell lines. The reported compounds have no structurally similarity to published structures, they are metabolically stable, have reasonable solubility and thus can serve as promising leads in the development of anticancer ATP-competitive inhibitors of human DNA topoisomerase IIα.
Language:
English
Keywords:
anticancer drugs
,
ATP-competitive inhibitors
,
catalytic inhibitor
,
cytotoxicity
,
human DNA topoisomerase II
Work type:
Article
Typology:
1.01 - Original Scientific Article
Organization:
FFA - Faculty of Pharmacy
Publication status:
Published
Publication version:
Version of Record
Year:
2023
Number of pages:
21 str.
Numbering:
Vol. 249, art. 115116
PID:
20.500.12556/RUL-144331
UDC:
577.27:615.28
ISSN on article:
0223-5234
DOI:
10.1016/j.ejmech.2023.115116
COBISS.SI-ID:
141491715
Publication date in RUL:
15.02.2023
Views:
751
Downloads:
104
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Record is a part of a journal
Title:
European journal of medicinal chemistry
Shortened title:
Eur. j. med. chem.
Publisher:
Elsevier
ISSN:
0223-5234
COBISS.SI-ID:
25429760
Licences
License:
CC BY 4.0, Creative Commons Attribution 4.0 International
Link:
http://creativecommons.org/licenses/by/4.0/
Description:
This is the standard Creative Commons license that gives others maximum freedom to do what they want with the work as long as they credit the author.
Secondary language
Language:
Slovenian
Keywords:
ATP-kompetitivni katalitični zaviralec
,
človeška DNA topoizomeraza II
,
rak
,
medicina
,
farmacevtska kemija
,
citotoksičnost
Projects
Funder:
ARRS - Slovenian Research Agency
Project number:
P1-0208
Name:
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin
Funder:
ARRS - Slovenian Research Agency
Project number:
N1-0172
Name:
Fotokemijski pristop za odkrivanje naprednih ATP-kompetitivnih prob z zaviralnim delovanjem na topoizomerazo II alfa
Funder:
Other - Other funder or multiple funders
Funding programme:
COST
Project number:
17104
Name:
New diagnostic and therapeutic tools against multidrug resistant tumors
Acronym:
STRATAGEM
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