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Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen - A new hybrid design paradigm.

Palermo, Anthony F; Diennet, Marine; El Ezzy, Mohamed; Williams, Benjamin M; Cotnoir-White, David; Mader, Sylvie; Gleason, James L.
Bioorg Med Chem; 26(15): 4428-4440, 2018 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-30078609
Hybrid antiestrogen/histone deacetylase (HDAC) inhibitors were designed by appending zinc binding groups to the 4-hydroxystilbene core of 4-hydroxytamoxifen. The resulting hybrids were fully bifunctional, and displayed high nanomolar to low micromolar IC50 values against both the estrogen receptor α (ERα) and HDACs in vitro and in cell-based assays. The hybrids were antiproliferative against ER+ MCF-7 breast cancer cells, with hybrid 28b possessing an improved activity profile compared to either 4-hydroxytamoxifen or SAHA. Hybrid 28b displayed gene expression patterns that reflected both ERα and HDAC inhibition.
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