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KMID : 0370220190630020113
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Yakhak Hoeji
2019 Volume.63 No. 2 p.113 ~ p.119
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Synthesis and DNA methyltransferase inhibitory activity of N,N'-(alkanediyl)bis(phenylacetamide) derivatives
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Lee So-Hyun
Ma Eun-Sook
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Abstract
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DNA methyltransferases (DNMTs) are epigenetic enzymes responsible for gene expression in cancer, therefore their inhibitors have been considered as target for the treatment and prevention of cancer. Psammaplin A (PsA) with dimeric disulfide structure exhibits excellent DNMT inhibitory activity, but there are synthetic limitations in the development of various derivatives. To develop various DNMT inhibitors that are easy to synthesize, N,N'-(alkanediyl) bis(phenylacetamide) derivatives 1-16 were synthesized from 3- or 4-substituted phenylacetic acids and α,ω-diaminoalkanes (NH2(CH2)nNH2, n=2-5) and evaluated for the preliminary screening of DNMT inhibitory activity using PsA as an positive control. The DNMT inhibitory activities (21-91%) of all synthesized compounds were lower than that of PsA (>100%) at 200 μM concentration. Among them, N,N'-(pentane-1,5-diyl)bis(2-(3-bromophenyl)acetamide) (12) was found to be most active compound with DNMT inhibition of 91%.
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KEYWORD
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DNA methyltransferase, N,N'-(alkanediyl)bis(phenylacetamide), epigenetics
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