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Title: Benzofuran-based estrogen receptor α modulators as anti-cancer therapeutics : in silico and experimental studies
Authors: Leow, Min Li
Chin, Christina Hui Li
Yu, Peggy Shuang
Pasunooti, Kalyan Kumar
Tay, Raymond Xu Zhan
Zhang, Dawei
Yoon, Ho Sup
Liu, Xue-Wei
Keywords: DRNTU::Science::Chemistry::Biochemistry
Issue Date: 2013
Source: Leow, 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.
Series/Report no.: Current medicinal chemistry
Abstract: In 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.
ISSN: 0929-8673
DOI: 10.2174/0929867311320220007
Fulltext Permission: none
Fulltext Availability: No Fulltext
Appears in Collections:SPMS Journal Articles

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