GENERAL ENQUIRIES: Tel: + 27 12 841 2911 | Email: callcentre@csir.co.za

Show simple item record

dc.contributor.author Wellington, Kevin W
dc.contributor.author Qwebani-Ogunleye, T
dc.contributor.author Kolesnikova, NI
dc.contributor.author Brady, D
dc.contributor.author De Koning, CB
dc.date.accessioned 2013-10-23T12:21:46Z
dc.date.available 2013-10-23T12:21:46Z
dc.date.issued 2013-04
dc.identifier.citation Wellington, K.W, Qwebani-Ogunleye, T, Kolesnikova, N.I, Brady, D and De Koning, C.B. 2013. A one-pot laccase-catalysed synthesis of 5,6-dihydroxylated benzo[b]furans and catechol derivatives, and their anticancer activity. Archive der Pharmazie Chemistry in Life Science, vol. 346, pp 266-277 en_US
dc.identifier.issn 0365-6233
dc.identifier.uri http://onlinelibrary.wiley.com/doi/10.1002/ardp.201200413/pdf
dc.identifier.uri http://hdl.handle.net/10204/7015
dc.description Copyright: 2013 Wiley Online Library. This is an ABSTRACT ONLY. The definitive version is published in Archive der Pharmazie Chemistry in Life Science, vol. 346, pp 266-277 en_US
dc.description.abstract 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. GI(sub)50, TGI and LC(sub)50 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 (GI9(sub50) = 0.77-9.76 (subµ)M) of which two compounds had better activity than the anticancer agent, etoposide (GI(sub50) = 0.89 (subµ)M). One compound exhibited potent activity (GI (sub50) = 9.73 (subµ) M) against the renal (TK10) cancer cell line and two exhibited potent activity (GI (sub50) = 8.79 and 9.30 (subµ)M) 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. en_US
dc.language.iso en en_US
dc.publisher Wiley Online Library en_US
dc.relation.ispartofseries Workflow;11569
dc.subject Laccase en_US
dc.subject Biocatalysis en_US
dc.subject Benzo[b]furans en_US
dc.subject C-C coupling en_US
dc.subject Catechols en_US
dc.subject 1,3-dicarbonyls en_US
dc.subject Michael addition en_US
dc.subject Anticancer en_US
dc.subject Cytostatic effects en_US
dc.subject Cytotoxic effects en_US
dc.title A one-pot laccase-catalysed synthesis of 5,6-dihydroxylated benzo[b]furans and catechol derivatives, and their anticancer activity en_US
dc.type Article en_US


Files in this item

This item appears in the following Collection(s)

Show simple item record

Search ResearchSpace


Advanced Search

Browse

My Account