afimoxifene and entinostat

afimoxifene has been researched along with entinostat* in 1 studies

Other Studies

1 other study(ies) available for afimoxifene and entinostat

Article	Year
Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids. Bioorganic & medicinal chemistry, 2015, Dec-15, Volume: 23, Issue:24 The combination of antiestrogens and histone deacetylase inhibitors (HDACi) has been found to be antiproliferative in breast cancer models. We designed and synthesized hybrid structures which combined structural features of the pure antiestrogen ICI-164,384 and HDACi's SAHA and entinostat in a single bifunctional molecule. The hybrids retained antiestrogenic and HDACi activity and, in the case of benzamide hybrids, were selective for Class I HDAC3 over Class II HDAC6. The hybrids possessed low micromolar to high nanomolar activity against both ER+ MCF-7 and ER- MDA-MB-231 breast cancer cell models. Topics: Antineoplastic Agents; Benzamides; Breast; Breast Neoplasms; Cell Line, Tumor; Estradiol; Estrogen Receptor Modulators; Female; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Molecular Docking Simulation; Polyunsaturated Alkamides; Pyridines	2015

Article

Year

Design, synthesis and evaluation of antiestrogen and histone deacetylase inhibitor molecular hybrids.

Bioorganic & medicinal chemistry, 2015, Dec-15, Volume: 23, Issue:24

The combination of antiestrogens and histone deacetylase inhibitors (HDACi) has been found to be antiproliferative in breast cancer models. We designed and synthesized hybrid structures which combined structural features of the pure antiestrogen ICI-164,384 and HDACi's SAHA and entinostat in a single bifunctional molecule. The hybrids retained antiestrogenic and HDACi activity and, in the case of benzamide hybrids, were selective for Class I HDAC3 over Class II HDAC6. The hybrids possessed low micromolar to high nanomolar activity against both ER+ MCF-7 and ER- MDA-MB-231 breast cancer cell models.

Topics: Antineoplastic Agents; Benzamides; Breast; Breast Neoplasms; Cell Line, Tumor; Estradiol; Estrogen Receptor Modulators; Female; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Molecular Docking Simulation; Polyunsaturated Alkamides; Pyridines

2015