Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells

New 6,N2-diaryl-1,3,5-triazine-2,4-diamines were designed using the 3D-QSAR model developed earlier. These compounds were prepared and their antiproliferative activity was evaluated against three breast cancer cell lines (MDA-MB231, SKBR-3 and MCF-7) and non-cancerous MCF-10A epithelial breast cell...

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Main Authors: Ahmad Junaid, Lim, Felicia Phei Lin, Tiekink, Edward R. T. *, Dolzhenko, Anton V
Format: Article
Language:English
Published: Royal Society of Chemistry 2020
Subjects:
Online Access:http://eprints.sunway.edu.my/1329/
http://eprints.sunway.edu.my/1329/1/Tiekink%20RSC%20Adv%202020%2010%2025517.pdf
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author Ahmad Junaid,
Lim, Felicia Phei Lin
Tiekink, Edward R. T. *
Dolzhenko, Anton V
author_facet Ahmad Junaid,
Lim, Felicia Phei Lin
Tiekink, Edward R. T. *
Dolzhenko, Anton V
author_sort Ahmad Junaid,
building SU Institutional Repository
collection Online Access
description New 6,N2-diaryl-1,3,5-triazine-2,4-diamines were designed using the 3D-QSAR model developed earlier. These compounds were prepared and their antiproliferative activity was evaluated against three breast cancer cell lines (MDA-MB231, SKBR-3 and MCF-7) and non-cancerous MCF-10A epithelial breast cells. The synthesized compounds demonstrated selective antiproliferative activity against triple negative MDA-MB231 breast cancer cells. The most active compound in the series inhibited MDA-MB231 breast cancer cell growth with a GI50 value of 1 nM. None of the tested compounds significantly affected the growth of the normal breast cells. The time-dependent cytotoxic effect, observed when cytotoxicity was assessed at different time intervals after the treatment, and morphological features, observed in the fluorescence microscopy and live cell imaging experiments, suggested apoptosis as the main pathway for the antiproliferative activity of these compounds against MDA-MB231 cells.
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spelling sunway-13292020-10-07T07:00:55Z http://eprints.sunway.edu.my/1329/ Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells Ahmad Junaid, Lim, Felicia Phei Lin Tiekink, Edward R. T. * Dolzhenko, Anton V RM Therapeutics. Pharmacology New 6,N2-diaryl-1,3,5-triazine-2,4-diamines were designed using the 3D-QSAR model developed earlier. These compounds were prepared and their antiproliferative activity was evaluated against three breast cancer cell lines (MDA-MB231, SKBR-3 and MCF-7) and non-cancerous MCF-10A epithelial breast cells. The synthesized compounds demonstrated selective antiproliferative activity against triple negative MDA-MB231 breast cancer cells. The most active compound in the series inhibited MDA-MB231 breast cancer cell growth with a GI50 value of 1 nM. None of the tested compounds significantly affected the growth of the normal breast cells. The time-dependent cytotoxic effect, observed when cytotoxicity was assessed at different time intervals after the treatment, and morphological features, observed in the fluorescence microscopy and live cell imaging experiments, suggested apoptosis as the main pathway for the antiproliferative activity of these compounds against MDA-MB231 cells. Royal Society of Chemistry 2020-06-28 Article PeerReviewed text en cc_by_nc_4 http://eprints.sunway.edu.my/1329/1/Tiekink%20RSC%20Adv%202020%2010%2025517.pdf Ahmad Junaid, and Lim, Felicia Phei Lin and Tiekink, Edward R. T. * and Dolzhenko, Anton V (2020) Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells. RSC Advances, 10. pp. 25517-25528. ISSN 2046-2069 (In Press) http://doi.org/10.1039/d0ra04970k doi:10.1039/d0ra04970k
spellingShingle RM Therapeutics. Pharmacology
Ahmad Junaid,
Lim, Felicia Phei Lin
Tiekink, Edward R. T. *
Dolzhenko, Anton V
Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells
title Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells
title_full Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells
title_fullStr Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells
title_full_unstemmed Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells
title_short Design, synthesis, and biological evaluation of new 6,N2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells
title_sort design, synthesis, and biological evaluation of new 6,n2-diaryl-1,3,5-triazine-2,4-diamines as anticancer agents selectively targeting triple negative breast cancer cells
topic RM Therapeutics. Pharmacology
url http://eprints.sunway.edu.my/1329/
http://eprints.sunway.edu.my/1329/
http://eprints.sunway.edu.my/1329/
http://eprints.sunway.edu.my/1329/1/Tiekink%20RSC%20Adv%202020%2010%2025517.pdf