Synthesis and anticancer activity of 6-heteroarylcoumarins.
Galayev O, Garazd Y, Garazd M, Lesyk R.
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).