2. Academic Validation
  3. Synthesis and growth inhibition activity of fluorinated derivatives of tamoxifen

Synthesis and growth inhibition activity of fluorinated derivatives of tamoxifen

  • Bioorg Med Chem Lett. 2013 Mar 15;23(6):1712-5. doi: 10.1016/j.bmcl.2013.01.057.
Bianca Malo-Forest 1,  Grégory Landelle,  Jessye-Ann Roy,  Jacques Lacroix,  René C Gaudreault,  Jean-François Paquin
Affiliations

Affiliation

  • 1 Canada Research Chair in Organic and Medicinal Chemistry, PROTEO, Département de Chimie, Université Laval, Québec, QC, Canada G1V 0A6.
PMID: 23403084 DOI: 10.1016/j.bmcl.2013.01.057
Abstract

The design and synthesis of 11 fluorinated derivatives of tamoxifen are described. Growth inhibition values (GI50) on human HT-29, M21, MCF7, and MDA-MB-231 tumor cells are also reported. In general, the GI50 values are similar or slightly higher than tamoxifen with the most active compound on MCF7 cell line having a GI50=3.6μM. Surprisingly, as opposed to tamoxifen, both geometrical isomers behave similarly. We hypothesize that this behavior is due to in vitro isomerization of the compounds.

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