115499-45-1Relevant articles and documents
Design and synthesis of novel benzothiophene analogs as selective estrogen receptor covalent antagonists against breast cancer
Bai, Chengfeng,Ren, Shengnan,Wu, Shuangjie,Zhu, Meiqi,Luo, Guoshun,Xiang, Hua
, (2021)
Endocrine therapy (ET) has benefited patients with estrogen receptor alpha (ERα) positive breast cancer for decades. Selective estrogen receptor modulator (SERM) such as Tamoxifen represents the clinical standard of care (SoC). Despite the therapeutic importance of current SoC agents, 30–50% of prolonged treatment patients inevitably generated resistant tumor cells, usually eventually suffered tumor relapse and developed into metastatic breast cancer (MBC), which was the leading cause of female cancer-related mortality. Among these, most resistant tumors remained dependent on ERα signaling, which reignited the need for the next generation of ERα related agents. We hypothesized that selective estrogen receptor covalent antagonists targeting ERα would provide a therapeutic alternative. In the current work, series of novel benzothiophene hybrids bearing electrophile moieties were synthesized and biologically evaluated. The representative analogue 15c exhibited potent anti-proliferative effect in MCF-7 cell lines in vitro, and further mechanism studies confirmed the necessity of covalent bonding. More importantly, 15c could attenuate the expression of TFF-1, GREB-1 and downregulate the levels of cellular ERα protein.
Anion-templated assembly of a [2]catenane
Sambrook, Mark R.,Beer, Paul D.,Wisner, James A.,Paul, Rowena L.,Cowley, Andrew R.
, p. 15364 - 15365 (2007/10/03)
The first example of a [2]catenane structure to be synthesized using anion templation is described. The nature of the anion template is demonstrated to be crucial to the assembly process, with only chloride anion producing the [2]catenane in acceptable yi
