Synthesis, anticancer and FGFR1 inhibitory activity of isoindolo[2,1-a][1,2,4]triazino[2,3-c]quinazoline derivatives
DOI:
https://doi.org/10.11603/mcch.2410-681X.2016.v0.i1.6123Abstract
Presented manuscript describes the synthesis, antitumor and FGFR1 inhibitory activity of novel isoindolo[2,1-a]
[1,2,4]triazino[2,3-c]quinazolines. It was shown that mentioned above substances may be prepared by interaction
of 3-(2-amino-3-R2-5-R3-phenyl)-6-R1-1,2,4-triazin-5(2H)-ones with 2-formylbenzoic and 6-formyl-2,3-dimethoxybenzoic (opianic) acids in acetic acid. It was shown that proper 2-(2-oxo-3-R-6,7-dihydro-2H-[1,2,4]triazino[2,3-c]quinazolin-
6-yl)benzoic acids (or corresponded dimethoxysubstituted analogues) may be considered as intermediates of the
reaction. Spectral properties of synthesized compounds were studied, it was shown that protons in position 8 were
observed at low field as result of the presence of hydrogen bond between hydrogen at position 8 and oxygen at
position 10. The anticancer assay data allowed to identify synthesized compounds as promising antitumor agents.
The FGFR1 inhibitory activity of synthesized compounds was detected and docking study aimed to the evaluation
of mentioned action was conducted.
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