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

Authors

  • O. Yu. Voskoboynik Zaporizhzhia State Medical University, Ukraine
  • I. S. Nosulenko Zaporizhzhia State Medical University, Ukraine
  • G. G. Berest Zaporizhzhia State Medical University, Ukraine
  • S. I. Kovalenko Zaporizhzhia State Medical University, Ukraine

DOI:

https://doi.org/10.24959/ubphj.16.29

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

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.

Author Biography

O. Yu. Voskoboynik, Zaporizhzhia State Medical University

завідувач кафедри органічної і біоорганічної хімії

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Published

2016-04-12

Issue

No. 2(43) (2016)

Section

Pharmaceutical chemistry and pharmacognosy

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