Synthesis and evaluation of anticancer activity of 6-pyrazolinylcoumarin derivatives.
A series of novel 6-pyrazolinylcoumarins has been synthesized via multi-step protocol. The synthetic procedure was based on the acetylation of hydroxycoumarins; Fries rearrangement and Claisen-Schmidt condensation; the target 6-[5-aryl-4,5-dihydropyrazol-3-yl]-5-hydroxy-7-methylcoumarins (33-49) were obtained under reactions of hydrazine and 2-aryl-5-methyl-2,3-dihydropyrano[2,3-f]chromen-4,8-diones as the last phase of the protocol. Anticancer activity screening in NCI60-cell lines assay allowed identification of compound47with the highest level of antimitotic activity with mean GI50value of 10.20 μM and certain sensitivity profile toward the Leukemia cell linesCCRF-CEMandMOLT-4(GI50/TGI values 1.88/5.06 μM and 1.92/4.04 μM respectively).
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.
Roman
R
Lesyk
Anticancer activity; Coumarins; Pyrazolines; Pyronoflavanones