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Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines

Quinazolines are known to be multitarget agents with broad spectrum of biological activity. Aim: To investigate anticancer activity of newly prepared 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline (BMAQ) towards L1210, HL-60 and U-937 leukemia cells. Materials and Methods: Growth inhibition of BMAQ...

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Main Authors: Jantova, S., Repicky, A., Paulovicova, E., Letasiova, S., Cipak, L.
Format: Article
Language:English
Published: Інститут експериментальної патології, онкології і радіобіології ім. Р.Є. Кавецького НАН України 2008
Series:Experimental Oncology
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Online Access:http://dspace.nbuv.gov.ua/handle/123456789/139208
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spelling irk-123456789-1392082018-06-20T03:12:30Z Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines Jantova, S. Repicky, A. Paulovicova, E. Letasiova, S. Cipak, L. Uncategorized Quinazolines are known to be multitarget agents with broad spectrum of biological activity. Aim: To investigate anticancer activity of newly prepared 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline (BMAQ) towards L1210, HL-60 and U-937 leukemia cells. Materials and Methods: Growth inhibition of BMAQ-treated cells was determined by cell counting using trypan blue staining technique. Apoptosis and cell cycle profile changes were analysed using internucleosomal DNA fragmentation assay, fluorescence microscopy and flow cytometry. Activity of caspase-3 was determined using colorimetric method. Results: Cell proliferation assay showed that BMAQ caused significant decrease of cell number in a dose-dependent manner. BMAQ induced cell death by apoptosis, based on results from DNA fragmentation, fluorescence microscopy and caspase-3 assays. Conclusion: Presented results clearly demonstrate that BMAQ is a promising anticancer agent with significant antiproliferative and apoptotic activities towards leukemia cells in vitro. Квиназолины известны как химиопрепараты широкого спектра действия. Цель: на моделях лейкозных клеток линий L1210, HL-60 и U-937 изучить противоопухолевую активность нового препарата 6-бромо-2-(морфолин-1-ил)-4-аналиноиназолина (BMAQ). Методы: ингибирование роста клеток под действием BMAQ изучали путем подсчета количества клеток, окрашенных трипановым синим. Апоптоз и изменения профиля клеточного цикла исследовали с помощью флуоресцентной микроскопии, электрофореза ДНК и проточной цитометрии. Активность каспазы-3 определяли колориметрическим методом. Результаты: показано, что BMAQ вызывает значительное дозозависимое уменьшение количества лейкозных клеток. При этом клетки, обработанные BMAQ, погибают путем апоптоза, что дается образованием апоптотических телец, межнуклеосомной фрагментацией ДНК и активацией каспазы-3. Выводы: представленные результаты свидетельствуют о том, что BMAQ обладает антипролиферативной и проапоптотической активностью в отношении лейкозных клеток in vitro. 2008 Article Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines / S. Jantova, A. Repicky, E. Paulovicova, S. Letasiova, L. Cipak // Experimental Oncology. — 2008. — Т. 30, № 2. — С. 139–142. — Бібліогр.: 17 назв. — англ. 1812-9269 http://dspace.nbuv.gov.ua/handle/123456789/139208 en Experimental Oncology Інститут експериментальної патології, онкології і радіобіології ім. Р.Є. Кавецького НАН України
institution Digital Library of Periodicals of National Academy of Sciences of Ukraine
collection DSpace DC
language English
topic Uncategorized
Uncategorized
spellingShingle Uncategorized
Uncategorized
Jantova, S.
Repicky, A.
Paulovicova, E.
Letasiova, S.
Cipak, L.
Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines
Experimental Oncology
description Quinazolines are known to be multitarget agents with broad spectrum of biological activity. Aim: To investigate anticancer activity of newly prepared 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline (BMAQ) towards L1210, HL-60 and U-937 leukemia cells. Materials and Methods: Growth inhibition of BMAQ-treated cells was determined by cell counting using trypan blue staining technique. Apoptosis and cell cycle profile changes were analysed using internucleosomal DNA fragmentation assay, fluorescence microscopy and flow cytometry. Activity of caspase-3 was determined using colorimetric method. Results: Cell proliferation assay showed that BMAQ caused significant decrease of cell number in a dose-dependent manner. BMAQ induced cell death by apoptosis, based on results from DNA fragmentation, fluorescence microscopy and caspase-3 assays. Conclusion: Presented results clearly demonstrate that BMAQ is a promising anticancer agent with significant antiproliferative and apoptotic activities towards leukemia cells in vitro.
format Article
author Jantova, S.
Repicky, A.
Paulovicova, E.
Letasiova, S.
Cipak, L.
author_facet Jantova, S.
Repicky, A.
Paulovicova, E.
Letasiova, S.
Cipak, L.
author_sort Jantova, S.
title Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines
title_short Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines
title_full Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines
title_fullStr Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines
title_full_unstemmed Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines
title_sort antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines
publisher Інститут експериментальної патології, онкології і радіобіології ім. Р.Є. Кавецького НАН України
publishDate 2008
topic_facet Uncategorized
url http://dspace.nbuv.gov.ua/handle/123456789/139208
citation_txt Antiproliferative activity and apoptosis induced by 6-bromo-2-(morpholin-1-yl)-4-anilinoquinazoline on cells of leukemia lines / S. Jantova, A. Repicky, E. Paulovicova, S. Letasiova, L. Cipak // Experimental Oncology. — 2008. — Т. 30, № 2. — С. 139–142. — Бібліогр.: 17 назв. — англ.
series Experimental Oncology
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AT letasiovas antiproliferativeactivityandapoptosisinducedby6bromo2morpholin1yl4anilinoquinazolineoncellsofleukemialines
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first_indexed 2023-10-18T21:19:52Z
last_indexed 2023-10-18T21:19:52Z
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