4.2 Article

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

Journal

MEDICINAL CHEMISTRY RESEARCH
Volume 21, Issue 5, Pages 552-558

Publisher

SPRINGER BIRKHAUSER
DOI: 10.1007/s00044-011-9562-z

Keywords

Antiestrogens; Antitumor; Prenylation; Xanthones

Funding

  1. FCT [4040, PTDC/SAU-FCT/100930/2008]
  2. COMPETE
  3. QREN
  4. FEDER
  5. POCI
  6. U. Porto
  7. Santander Totta

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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 (GI(50) = 5 mu M), showed an enhancement in the anti-estrogenic effect of 4-hydroxytamoxifen in this ER(+) cell line.

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