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Updated: Mar 31, 2026

Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
Published on: June 26, 2018
Synthesis and anticancer activity of 6-heteroarylcoumarins
Olexandr Galayev1, Yana Garazd1, Myroslav Garazd1
1Eximed, Kharkivske shose 50, Kyiv, 02160, Ukraine.
Abstract:
A series of novel 7-hydroxy-8-methyl-coumarins with indole, pyrimidine, pyrazole, pyran, tetrazolo[1,5-a]pyrimidine, pyrimido[1,2-a]benzimidazol, 2-oxo-1,2-dihydropyridine and dihydropyrazolo[3,4-b]pyridine moieties at C6 position of heterocyclic core have been synthesized. Anticancer activity screening on NCI60 cell lines allowed identification of 6-(6-fluoro-1H-indol-2-yl)-7-hydroxy-4,8-dimethyl-2H-chromen-2-one (23) with the highest level of antimitotic activity with mean GI50/TGI values of 3.28/13.24 μM and certain sensitivity profile towards the Non-Small Cell Lung Cancer cell line НОР-92 (GI50/TGI/LC50 values 0.95/4.17/29.9 μM).
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