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Issue 48, 2012
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Discovery of novel SERMs with a ferrocenyl entity based on the oxabicyclo[2.2.1]heptene scaffold and evaluation of their antiproliferative effects in breast cancer cells

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Abstract

We have synthesized a series of novel SERMs bearing a ferrocenyl unit based on a three-dimensional oxabicyclo[2.2.1]heptene core scaffold. These compounds displayed high receptor binding affinities as well as ERα or ERβ selectivity. In cell proliferation assays, we found that these ligands were cytotoxic at micromolar concentrations in both ER-positive and ER-negative breast cancer cells. On further examination, we found that the antiproliferative effects of compounds 9b, 10h and 11b on MCF-7 cells line does not arise from antiestrogenicity, but rather proceeds through a cytotoxic pathway. Possible mechanisms for the unique activities of these ligands were also investigated by molecular modeling. These new ligands could act as scaffolds for the development of novel anti-breast cancer agents.

Graphical abstract: Discovery of novel SERMs with a ferrocenyl entity based on the oxabicyclo[2.2.1]heptene scaffold and evaluation of their antiproliferative effects in breast cancer cells

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Publication details

The article was received on 27 Jun 2012, accepted on 23 Oct 2012 and first published on 24 Oct 2012


Article type: Paper
DOI: 10.1039/C2OB26226F
Citation: Org. Biomol. Chem., 2012,10, 9689-9699
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    Discovery of novel SERMs with a ferrocenyl entity based on the oxabicyclo[2.2.1]heptene scaffold and evaluation of their antiproliferative effects in breast cancer cells

    Y. Zheng, C. Wang, C. Li, J. Qiao, F. Zhang, M. Huang, W. Ren, C. Dong, J. Huang and H. Zhou, Org. Biomol. Chem., 2012, 10, 9689
    DOI: 10.1039/C2OB26226F

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