Synthesis and anticancer activity of 6-heteroarylcoumarins.
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).
Eximed, Kharkivske shose 50, Kyiv, 02160, Ukraine.
Olexandr
O
Galayev
Eximed, Kharkivske shose 50, Kyiv, 02160, Ukraine.
Yana
Y
Garazd
Eximed, Kharkivske shose 50, Kyiv, 02160, Ukraine.
Myroslav
M
Garazd
Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, Lviv, 79010, Ukraine. Electronic address: dr_r_lesyk@org.lviv.net.
Roman
R
Lesyk
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D003374:Coumarins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D003374:Coumarins
6-Heteroarylcoumarins; Anticancer activity; Synthesis