Tag Archives: 5-amino-1-aryl-1H-1

Selected 5-amino-1-aryl-1H-1,2,3-triazole scaffolds as promising antiproliferative agents

N. Pokhodylo1*, O. Shyyka1, N. Finiuk2, R. Stoika2

1Ivan Franko National University of Lviv, Ukraine;
2Institute of Cell Biology, National Academy of Sciences of Ukraine, Lviv;
*e-mail: pokhodylo@gmail.com; stoika@cellbiol.lviv.ua

Received: 09 January 2020; Accepted: 25 June 2020

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.