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首页> 外文期刊>Archiv der Pharmazie >One-pot laccase-catalysed synthesis of 5,6-dihydroxylated benzo[b]furans and catechol derivatives, and their anticancer activity
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One-pot laccase-catalysed synthesis of 5,6-dihydroxylated benzo[b]furans and catechol derivatives, and their anticancer activity

机译：一锅漆酶催化的5,6-二羟基化苯并[b]呋喃和邻苯二酚衍生物的合成及其抗癌活性

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摘要

A commercial laccase, Suberase? from Novozymes, was used to catalyse the synthesis of 5,6-dihydroxylated benzo[b]furans and catechol derivatives. The yields were, in some cases, similar to or better than that obtained by other enzymatic, chemical or electrochemical syntheses. The synthesised derivatives were screened against renal (TK10), melanoma (UACC62), breast (MCF7) and cervical (HeLa) cancer cell lines. GI50, TGI and LC50 are reported for the first time. Anticancer screening showed that the cytostatic effects of the 5,6-dihydroxylated benzo[b]furans were most effective against the melanoma (UACC62) cancer cell line with several compounds exhibiting potent growth inhibitory activities (GI50 = 0.77-9.76 μM), of which two compounds had better activity than the anticancer agent etoposide (GI 50 = 0.89 μM). One compound exhibited potent activity (GI 50 = 9.73 μM) against the renal (TK10) cancer cell line and two exhibited potent activity (GI50 = 8.79 and 9.30 μM) against the breast (MCF7) cancer cell line. These results encourage further studies of the 5,6-dihydroxylated benzo[b]furans for their potential application in anticancer therapy. The anticancer activities of a series of enzyme-catalysed 5,6-dihydroxylated benzo[b]furans were assessed. The cytostatic effects of the 5,6-dihydroxylated benzo[b]furans were highest against the melanoma cancer cell line UACC62, with several compounds exhibiting potent growth inhibitory activities (GI50 = 0.77-9.76 μM). Two compounds had better activity than the anticancer agent etoposide (GI50 = 0.89 μM).
机译：商业漆酶，Suberase？诺维信公司（Novozymes）生产的Nanozyme用于催化5，6-二羟基化苯并[b]呋喃和邻苯二酚衍生物的合成。在某些情况下，产率类似于或优于通过其他酶，化学或电化学合成获得的产率。筛选了针对肾（TK10），黑素瘤（UACC62），乳腺癌（MCF7）和宫颈癌（HeLa）癌细胞系的合成衍生物。 GI50，TGI和LC50首次报告。抗癌筛选显示，5,6-二羟基化苯并[b]呋喃的细胞抑制作用对黑素瘤（UACC62）癌细胞系最有效，其中几种化合物具有有效的生长抑制活性（GI50 = 0.77-9.76μM），其中两种化合物的活性均优于抗癌药依托泊苷（GI 50 = 0.89μM）。一种化合物对肾（TK10）癌细胞系表现出有效的活性（GI 50 = 9.73μM），而两种化合物对乳腺癌（MCF7）癌细胞系表现出有效的活性（GI50 = 8.79和9.30μM）。这些结果鼓励了对5,6-二羟基化苯并[b]呋喃在抗癌治疗中的潜在应用的进一步研究。评估了一系列酶催化的5，6-二羟基化苯并[b]呋喃的抗癌活性。 5，6-二羟基化苯并[b]呋喃对黑色素瘤癌细胞系UACC62的抑制作用最高，几种化合物均表现出有效的生长抑制活性（GI50 = 0.77-9.76μM）。两种化合物的活性均优于抗癌药依托泊苷（GI50 = 0.89μM）。

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