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Prenylated xanthones: antiproliferative effects and enhancement of the growth inhibitory action of 4-hydroxytamoxifen in estrogen receptor-positive breast cancer cell line

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Abstract

The effects of three prenylated xanthones on the in vitro growth of estrogen-dependent ER (+) MCF-7 (breast), estrogen-independent ER (−) MDA-MB-231 cells (breast), and NCI-H460 (non-small cell lung) were investigated in a complete and/or steroid-free medium. 3,4-Dihydro-12-hydroxy-2,2-dimethyl-2H,6H-pyrano[3,2-b]xanthen-6-one (4), the most potent against the ER(+) MCF-7 cell line (GI50 = 5 μM), showed an enhancement in the anti-estrogenic effect of 4-hydroxytamoxifen in this ER(+) cell line.

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Acknowledgments

This study was supported by FCT [I&D, no. 4040 and PTDC/SAU-FCT/100930/2008], COMPETE, QREN, FEDER, POCI, U. Porto, and Santander Totta. The authors are also indebted to the National Cancer Institute, Bethesda, MD, USA, for the generous provision of the human tumor cell lines and to Sara Cravo for technical support in spectroscopic methods.

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Authors and Affiliations

  1. Department of Chemistry, Laboratory of Organic and Pharmaceutical Chemistry, Faculty of Pharmacy, University of Porto, Rua Aníbal Cunha 164, 4050-047, Porto, Portugal

    Ana Mafalda Paiva, Maria Emília Sousa & Madalena Maria Magalhães Pinto

  2. Research Center of Medicinal Chemistry (CEQUIMED-UP), University of Porto, Rua Aníbal Cunha 164, 4050-047, Porto, Portugal

    Ana Mafalda Paiva, Maria Emília Sousa, Ana Camões, Maria São José Nascimento & Madalena Maria Magalhães Pinto

  3. Department of Biological Sciences, Faculty of Pharmacy, University of Porto, Rua Anibal Cunha 164, 4050-047, Porto, Portugal

    Ana Camões & Maria São José Nascimento

Authors
  1. Ana Mafalda Paiva
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  2. Maria Emília Sousa
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  3. Ana Camões
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  4. Maria São José Nascimento
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  5. Madalena Maria Magalhães Pinto
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Correspondence to Madalena Maria Magalhães Pinto.

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Paiva, A.M., Sousa, M.E., Camões, A. et al. Prenylated xanthones: antiproliferative effects and enhancement of the growth inhibitory action of 4-hydroxytamoxifen in estrogen receptor-positive breast cancer cell line. Med Chem Res 21, 552–558 (2012). https://doi.org/10.1007/s00044-011-9562-z

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  • DOI: https://doi.org/10.1007/s00044-011-9562-z

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