dc.contributor.author | Wellington, Kevin W. | |
dc.contributor.author | Motadi, Lesetja R. | |
dc.contributor.author | Kolesnikova, Natasha I. | |
dc.contributor.author | Hlatshwayo, Vincent | |
dc.contributor.author | Saha, Sourav T. | |
dc.date.accessioned | 2020-06-18T13:09:15Z | |
dc.date.available | 2020-06-18T13:09:15Z | |
dc.date.issued | 2020 | |
dc.identifier.citation | Wellington, K.W. et al. 2020. Anticancer activity, apoptosis and a structure–activity analysis of a series of 1,4-naphthoquinone-2,3-bis-sulfides. Investigational new drugs, 38(2):274-286. [https://doi.org/10.1007/s10637-019-00775-7] | en_US |
dc.identifier.issn | 0167-6997 | |
dc.identifier.issn | 1573-0646 (Online) | |
dc.identifier.uri | http://hdl.handle.net/10394/34795 | |
dc.identifier.uri | https://link.springer.com/article/10.1007/s10637-019-00775-7 | |
dc.identifier.uri | https://doi.org/10.1007/s10637-019-00775-7 | |
dc.description.abstract | We have previously reported on the synthesis of 1,4-naphthoquinone-sulfides and in this investigation we report on their anticancer activity against 6 human cancer cell lines to evaluate their cytostatic effects. The 1,4-naphthoquinone-2,3-bis-sulfides were most effective against melanoma (UACC62) (GI50 = 6.5–10 μM) and prostate (PC3) (GI50 = 5.51–8.53 μM) cancer cell lines. They exhibited better cytostatic effects than etoposide (GI50 = 0.56–36.62 μM), parthenolide (GI50 = 3.58–25.97 μM) and VK3 (GI50 = 3.41–22.59 μM) against several of the cancer cell lines. These compounds are generally more selective for cancer cells than for normal human lung fetal fibroblasts (WI-38). One compound produces ROS which results in breast (MCF7) cancer cell death caused by apoptosis as evidenced by caspase 3/7 activation. Apoptosis was found to occur by a mitochondrial pathway and not by cell cycle arrest. Gene expression studies showed that p53 (a tumour suppressor), Mdm-2 (a p53 regulator) and Bcl-2 (apoptosis inhibitor) were up-regulated during apoptosis induction. These results encourage further research for potential application in cancer chemotherapy | en_US |
dc.language.iso | en | en_US |
dc.publisher | Springer | en_US |
dc.subject | 1,4-Naphthoquinone-2,3-bis-sulfides | en_US |
dc.subject | Melanoma cancer | en_US |
dc.subject | Breast cancer | en_US |
dc.subject | Prostate cancer | en_US |
dc.subject | Apoptosis | en_US |
dc.title | Anticancer activity, apoptosis and a structure-activity analysis of a series of 1,4-naphthoquinone-2,3-bis-sulfides | en_US |
dc.type | Article | en_US |
dc.contributor.researchID | 27616002 - Motadi, Lesetja Raymond | |