TY - JOUR
T1 - Anti-cancer activity of phenyl and pyrid-2-yl 1,3-substituted benzo[1,2,4]triazin-7-ones and stable free radical precursors
AU - Keane, Lee Ann J.
AU - Mirallai, Styliana I.
AU - Sweeney, Martin
AU - Carty, Michael P.
AU - Zissimou, Georgia A.
AU - Berezin, Andrey A.
AU - Koutentis, Panayiotis A.
AU - Aldabbagh, Fawaz
N1 - Publisher Copyright:
© 2018 by the authors.
PY - 2018
Y1 - 2018
N2 - Cell viability studies for benzo[1,2,4]triazin-7-ones and 1,2,4-benzotriazinyl (Blatter-type) radical precursors are described with comparisons made with 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). All of the stable free radicals were several orders of magnitude less cytotoxic than the benzo[1,2,4] triazin-7-ones. The synthesis and evaluation of two new pyrid-2-yl benzo[1,2,4] triazin-7-ones are described, where altering the 1,3-substitution from phenyl to pyrid-2-yl increased cytotoxicity against most cancer cell lines, as indicated using National Cancer Institute (NCI) one-dose testing. COMPARE analysis of five-dose testing data from the NCI showed very strong correlations to the naturally occurring anti-cancer compound pleurotin. COMPARE is program, which analyzes similarities in cytotoxicity data of compounds, and enables quantitative expression as Pearson correlation coefficients. Compounds were also evaluated using the independent MTT assay, which was compared with SRB assay data generated at the NCI.
AB - Cell viability studies for benzo[1,2,4]triazin-7-ones and 1,2,4-benzotriazinyl (Blatter-type) radical precursors are described with comparisons made with 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). All of the stable free radicals were several orders of magnitude less cytotoxic than the benzo[1,2,4] triazin-7-ones. The synthesis and evaluation of two new pyrid-2-yl benzo[1,2,4] triazin-7-ones are described, where altering the 1,3-substitution from phenyl to pyrid-2-yl increased cytotoxicity against most cancer cell lines, as indicated using National Cancer Institute (NCI) one-dose testing. COMPARE analysis of five-dose testing data from the NCI showed very strong correlations to the naturally occurring anti-cancer compound pleurotin. COMPARE is program, which analyzes similarities in cytotoxicity data of compounds, and enables quantitative expression as Pearson correlation coefficients. Compounds were also evaluated using the independent MTT assay, which was compared with SRB assay data generated at the NCI.
KW - Anti-tumour
KW - Blatter-type radical
KW - Heterocyclic compound
KW - NCI
KW - Pleurotin
KW - TEMPO
UR - https://www.scopus.com/pages/publications/85043473150
U2 - 10.3390/molecules23030574
DO - 10.3390/molecules23030574
M3 - Article
SN - 1420-3049
VL - 23
JO - Molecules
JF - Molecules
IS - 3
M1 - 574
ER -
