186787-88-2Relevant academic research and scientific papers
A Chimeric SERM-histone deacetylase inhibitor approach to breast cancer therapy
Patel, Hitisha K.,Siklos, Marton I.,Abdelkarim, Hazem,Mendonca, Emma L.,Vaidya, Aditya,Petukhov, Pavel A.,Thatcher, Gregory R. J.
, p. 602 - 613 (2014/03/21)
Breast cancer remains a significant cause of death in women, and few therapeutic options exist for estrogen receptor negative (ER (-)) cancers. Epigenetic reactivation of target genes using histone deacetylase (HDAC) inhibitors has been proposed in ER (-) cancers to resensitize to therapy using selective estrogen receptor modulators (SERMs) that are effective in ER (+) cancer treatment. Based upon preliminary studies in ER (+) and ER (-) breast cancer cells treated with combinations of HDAC inhibitors and SERMs, hybrid drugs, termed SERMostats, were designed with computational guidance. Assay for inhibition of four typea I HDAC isoforms and antagonism of estrogenic activity in two cell lines yielded a SERMostat with 1-3a μM potency across all targets. The superior hybrid caused significant cell death in ER (-) human breast cancer cells and elicited cell death at the same concentration as the parent SERM in combination treatment and at an earlier time point.
Acrylic and propionic acid compounds, intermediates, processes, compositions, and method
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Page column 8, (2010/01/30)
This invention is directed to a class of acrylic and propionic acid compounds and their use in the treatment of post-menopausal symptoms and restenosis. In other embodiments, the invention is directed to intermediates and to processes for the preparation of the acrylic and propionic acid compounds.
Intermediates and processes for preparing benzo (b) thiophenes
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, (2008/06/13)
The instant invention provides processes for preparing compounds of formula IV, V, and IX, having the structures provided hereinbelow: These compounds are useful intermediates in the further preparation of benzo[b] thiophenes.
