CSIR Biosciences, Pretoria, South Africa.
Arch Pharm (Weinheim). 2013 Apr;346(4):266-77. doi: 10.1002/ardp.201200413. Epub 2013 Feb 28.
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 (GI50 0.89 µM). One compound exhibited potent activity (GI50=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.
商业漆酶 Suberase®（来自诺维信）被用于催化 5,6-二羟基苯并呋喃和儿茶酚衍生物的合成。在某些情况下，产率与其他酶法、化学法或电化学法合成相当或更好。所合成的衍生物对肾（TK10）、黑色素瘤（UACC62）、乳腺（MCF7）和宫颈（HeLa）癌细胞系进行了筛选。首次报道了 GI50、TGI 和 LC50。抗癌筛选表明，5,6-二羟基苯并呋喃的细胞抑制作用对黑色素瘤（UACC62）癌细胞系最为有效，其中几种化合物具有很强的生长抑制活性（GI50=0.77-9.76 μM），其中两种化合物的活性优于抗癌药物依托泊苷（GI50=0.89 μM）。一种化合物对肾（TK10）癌细胞系具有很强的活性（GI50=9.73 μM），两种化合物对乳腺（MCF7）癌细胞系具有很强的活性（GI50=8.79 和 9.30 μM）。这些结果鼓励进一步研究 5,6-二羟基苯并呋喃在抗癌治疗中的潜在应用。
