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Synthesis and evaluation of anticancer activity of 6-pyrazolinylcoumarin derivatives.

ABSTRACT: 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 compound 47 with the highest level of antimitotic activity with mean GI₅₀ value of 10.20 ?M and certain sensitivity profile toward the Leukemia cell lines CCRF-CEM and MOLT-4 (GI₅₀/TGI values 1.88/5.06 ?M and 1.92/4.04 ?M respectively).

SUBMITTER: Garazd Y

PROVIDER: S-EPMC5355548 | biostudies-literature | 2017 Feb

REPOSITORIES: biostudies-literature

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Synthesis and evaluation of anticancer activity of 6-pyrazolinylcoumarin derivatives.

Garazd Yana Y Garazd Myroslav M Lesyk Roman R

Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society 20160603 2

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 (<b>33-49</b>) were obtained under reactions of hydrazine and 2-aryl-5-methyl-2,3-dihydropyrano[2,3-<i>f</i>]chromen-4,8-diones as the last phase of the protocol. Anticancer activity screening in NCI60-cell line ...[more]

PMID: 28344471

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