6-Mono- and 6,6-disubstituted 3-r-6,7-dihydro-2h-[1,2,4]-triazino[2,3-c]quinazoline-2-ones – promising class of anticancer agents

O. Yu. Voskoboynik, I. S. Nosulenko, G. G. Berest, S. I. Kovalenko

Abstract


Anticancer activity of novel 6-mono- and 6,6-disubstituted  3-R-6,7-dihydro-2H-[1,2,4]triazino[2,3-c]quinazolin-2-ones was described in presented manuscript. It was shown, that 10-bromo-6-isobutyl-3-(4-fluorophenyl)-6,7-dihydro-2H-[1,2,4]-triazino-[2,3-c]quinazolin-2-one (1.3) and 6-(methoxyphenyl)-8-methyl-3-phenyl-6,7-dihydro-2H-[1,2,4]-triazino-[2,3-c]-quinazolin-2-one (1.4) reveals high non-selective anticancer activity (mean growth -10.53 and 46.24% correspondingly) against 60 cancer cell lines. Substantial dose-depended iv vitro study on 60 cancer cell lines for compound 1.3 showed, that it effectively inhibits growth of SR (lg GI50 = -6,17) of leukemia, NCI-H460 (lg GI50 = -5,79) of non-small lung cancer, HCT-116 (lg GI50 = -5,80), HCT-15 (lg GI50 = -5,78) of colon cancer, SNB-75 (lg GI50 = -5,88), U-251 (lg GI50 = -5,81) of CNS cancer, UACC-257 (lg GI50 = -5,83), UACC-62 (lg GI50 = -5,81) of melanoma, A498 (lg GI50 = -5,80), UO-31 (lg GI50 = -5,81) of renal cancer and MDA-MB-231/ATCC (lg GI50 = -5,81), MDA-MB-468 (lg GI50 = -5,80) of breast cancer cell lines. “Structure-biological activity” relationships for described compounds were discussed.

Keywords


6-mono- і 6,6-disubstituted 3-R-6,7-dihydro-2H-[1,2,4]triazino[2,3-c]quinazoline-2-ones; in vitro screening; anticancer activity

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References


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DOI: https://doi.org/10.24959/89826

Abbreviated key title: Ukr. bìofarm. ž.

ISSN 2519-8750 (Online), ISSN 2311-715X (Print)