Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents
Development of a new effective drugs with low side effects and definite chemical characteristics needs indentification of bioactive scaffolds for further structural optimization. New synthesized derivatives of 4-hetaryl-5-amino-1-aryl-1H-1,2,3-triazoles and 3H-[1,2,3]triazolo[4,5-b]pyridines were te...
Main Authors: | , , , |
---|---|
Format: | Article |
Language: | English |
Published: |
National Academy of Sciences of Ukraine and Palladin Institute of Biochemistry of the National Academy of Sciences of Ukraine.
2020-10-01
|
Series: | Ukrainian Biochemical Journal |
Subjects: | |
Online Access: | http://ukrbiochemjournal.org/wp-content/uploads/2020/11/Pokhodylo_5_20.pdf |
id |
doaj-ce1c931a465e46d9b390c16609415695 |
---|---|
record_format |
Article |
spelling |
doaj-ce1c931a465e46d9b390c166094156952021-02-19T10:43:40ZengNational Academy of Sciences of Ukraine and Palladin Institute of Biochemistry of the National Academy of Sciences of Ukraine.Ukrainian Biochemical Journal2409-49432413-50032020-10-01925233210.15407/ubj92.05.023Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agentsN. Pokhodylo0https://orcid.org/0000-0001-8222-5008O. Shyyka1https://orcid.org/0000-0003-4513-6385N. Finiuk2https://orcid.org/0000-0002-4112-8815R. Stoika3https://orcid.org/0000-0001-5719-2187Ivan Franko National University of Lviv, UkraineIvan Franko National University of Lviv, UkraineInstitute of Cell Biology, National Academy of Sciences of Ukraine, LvivInstitute of Cell Biology, National Academy of Sciences of Ukraine, LvivDevelopment of a new effective drugs with low side effects and definite chemical characteristics needs indentification of bioactive scaffolds for further structural optimization. New synthesized derivatives of 4-hetaryl-5-amino-1-aryl-1H-1,2,3-triazoles and 3H-[1,2,3]triazolo[4,5-b]pyridines were tested for anticancer activity using 60 human tumor cell lines within 9 cancer types. The selective influence of (5-amino-1H-1,2,3-triazol-4-yl)quinazolin-4(3H)-ones: 2-(5-amino-1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)quinazolin-4(3H)-one and 2-(5-amino-1-phenyl-1H-1,2,3-triazol-4-yl)-6-bromoquinazolin-4(3H)-one on ovarian cancer OVCAR-4 cells with growth percentage (GP) = -4.08 and 6.63%, respectively, was found. The derivative 5,7-diamino-3-(3-(trifluoromethyl)phenyl)-3H-[1,2,3]triazolo[4,5-b]pyridine-6-carbonitrile possessed high activity towards lung cancer EKVX cells (GP = 29.14%). The compounds were shown to be less toxic than doxorubicin towards non-tumor human embryonic kidney cells of HEK293 line. Thus, the results of our study confirm the anticancer potential of compounds based on 5-amino-1-aryl-1H-1,2,3-triazoles scaffolds and their fused polycyclic derivatives.http://ukrbiochemjournal.org/wp-content/uploads/2020/11/Pokhodylo_5_20.pdf5-amino-1-aryl-1h-1;2;3-triazoles3h-[1;2;3]triazolo[4;5-b]pyridinesquinazolinonesthiazoles1;3;4-oxadiazolesantiproliferative activityanticancer activity |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
N. Pokhodylo O. Shyyka N. Finiuk R. Stoika |
spellingShingle |
N. Pokhodylo O. Shyyka N. Finiuk R. Stoika Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents Ukrainian Biochemical Journal 5-amino-1-aryl-1h-1;2;3-triazoles 3h-[1;2;3]triazolo[4;5-b]pyridines quinazolinones thiazoles 1;3;4-oxadiazoles antiproliferative activity anticancer activity |
author_facet |
N. Pokhodylo O. Shyyka N. Finiuk R. Stoika |
author_sort |
N. Pokhodylo |
title |
Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents |
title_short |
Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents |
title_full |
Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents |
title_fullStr |
Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents |
title_full_unstemmed |
Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents |
title_sort |
selected 5-amino-1-aryl-1h-1,2,3-triazole scaffolds as promising antiproliferative agents |
publisher |
National Academy of Sciences of Ukraine and Palladin Institute of Biochemistry of the National Academy of Sciences of Ukraine. |
series |
Ukrainian Biochemical Journal |
issn |
2409-4943 2413-5003 |
publishDate |
2020-10-01 |
description |
Development of a new effective drugs with low side effects and definite chemical characteristics needs indentification of bioactive scaffolds for further structural optimization. New synthesized derivatives of 4-hetaryl-5-amino-1-aryl-1H-1,2,3-triazoles and 3H-[1,2,3]triazolo[4,5-b]pyridines were tested for anticancer activity using 60 human tumor cell lines within 9 cancer types. The selective influence of (5-amino-1H-1,2,3-triazol-4-yl)quinazolin-4(3H)-ones: 2-(5-amino-1-(4-chlorophenyl)-1H-1,2,3-triazol-4-yl)quinazolin-4(3H)-one and 2-(5-amino-1-phenyl-1H-1,2,3-triazol-4-yl)-6-bromoquinazolin-4(3H)-one on ovarian cancer OVCAR-4 cells with growth percentage (GP) = -4.08 and 6.63%, respectively, was found. The derivative 5,7-diamino-3-(3-(trifluoromethyl)phenyl)-3H-[1,2,3]triazolo[4,5-b]pyridine-6-carbonitrile possessed high activity towards lung cancer EKVX cells (GP = 29.14%). The compounds were shown to be less toxic than doxorubicin towards non-tumor human embryonic kidney cells of HEK293 line. Thus, the results of our study confirm the anticancer potential of compounds based on 5-amino-1-aryl-1H-1,2,3-triazoles scaffolds and their fused polycyclic derivatives. |
topic |
5-amino-1-aryl-1h-1;2;3-triazoles 3h-[1;2;3]triazolo[4;5-b]pyridines quinazolinones thiazoles 1;3;4-oxadiazoles antiproliferative activity anticancer activity |
url |
http://ukrbiochemjournal.org/wp-content/uploads/2020/11/Pokhodylo_5_20.pdf |
work_keys_str_mv |
AT npokhodylo selected5amino1aryl1h123triazolescaffoldsaspromisingantiproliferativeagents AT oshyyka selected5amino1aryl1h123triazolescaffoldsaspromisingantiproliferativeagents AT nfiniuk selected5amino1aryl1h123triazolescaffoldsaspromisingantiproliferativeagents AT rstoika selected5amino1aryl1h123triazolescaffoldsaspromisingantiproliferativeagents |
_version_ |
1724261317849645056 |