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dc.contributor.authorLeow, Min Lien
dc.contributor.authorChin, Christina Hui Lien
dc.contributor.authorYu, Peggy Shuangen
dc.contributor.authorPasunooti, Kalyan Kumaren
dc.contributor.authorTay, Raymond Xu Zhanen
dc.contributor.authorZhang, Daweien
dc.contributor.authorYoon, Ho Supen
dc.contributor.authorLiu, Xue-Weien
dc.identifier.citationLeow, M. L., Chin, C. H. L., Yu, P. S., Pasunooti, K. K., Tay, R. X. Z., Zhang, D., et al. (2013). Benzofuran-based estrogen receptor α modulators as anti-cancer therapeutics : in silico and experimental studies. Current medicinal chemistry, 20(22), 2820-2837.en
dc.description.abstractIn the search for new estrogen receptor alpha (ERα) modulators, a trial molecular screening was conducted and 5,6-dihydroxybenzofuran was identified as a possible drug target for ERα. The target molecular modelling molecule 1 and a series of 5,6-dihydroxybenzofurans have been synthesized and evaluated for their anti-proliferation activities against MCF-7 and MDA-MB-231 cells. From the SAR studies, potential functional groups have been identified, the two hydroxyl groups at C-5 and C-6 and the phenyl ring at C-2, which showed considerable cytotoxicity in MCF-7 breast cancer cells. In addition, the apoptotic abilities of the compounds have been measured in both MCF-7 ER(+) and MDA-MB-231 ER(-) breast cancer cells. The results demonstrated that our compounds inhibit MCF-7 breast cancer cells via ER(+). These preliminary results provide valuable information towards the identification of important functional groups present on 5,6-dihydroxybenzofuran, which could be a promising scaffold for designing novel ER ligands.en
dc.relation.ispartofseriesCurrent medicinal chemistryen
dc.titleBenzofuran-based estrogen receptor α modulators as anti-cancer therapeutics : in silico and experimental studiesen
dc.typeJournal Articleen
dc.contributor.schoolSchool of Physical and Mathematical Sciencesen
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