Synthesis and anticancer activity of 6-heteroarylcoumarins

Olexandr Galayev; Yana Garazd; Myroslav Garazd; Roman Lesyk

doi:10.1016/j.ejmech.2015.10.021

Synthesis and anticancer activity of 6-heteroarylcoumarins

Eur J Med Chem. 2015 Nov 13:105:171-81. doi: 10.1016/j.ejmech.2015.10.021. Epub 2015 Oct 24.

Authors

Olexandr Galayev¹, Yana Garazd¹, Myroslav Garazd¹, Roman Lesyk²

Affiliations

¹ Eximed, Kharkivske shose 50, Kyiv, 02160, Ukraine.
² 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.

PMID: 26491980
DOI: 10.1016/j.ejmech.2015.10.021

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).

Keywords: 6-Heteroarylcoumarins; Anticancer activity; Synthesis.

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Cell Proliferation / drug effects
Cell Survival / drug effects
Coumarins / chemical synthesis
Coumarins / chemistry
Coumarins / pharmacology*
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Structure-Activity Relationship

Substances

Antineoplastic Agents
Coumarins