Design and synthesis of novel benzothiophene analogs as selective estrogen receptor covalent antagonists against breast cancer was written by Bai, Chengfeng;Ren, Shengnan;Wu, Shuangjie;Zhu, Meiqi;Luo, Guoshun;Xiang, Hua. And the article was included in European Journal of Medicinal Chemistry in 2021.Recommanded Product: 4-Benzyloxyphenol The following contents are mentioned in the article:
Endocrine therapy (ET) has benefited patients with estrogen receptor alpha (ERα) pos. breast cancer for decades. Selective estrogen receptor modulator (SERM) such as Tamoxifen represents the clin. 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. Authors hypothesized that selective estrogen receptor covalent antagonists targeting ERα would provide a therapeutic alternative. In the current work, series of novel benzothiophene hybrids I (R1 = H, Me; R2 = Me; R1R2 = (CH2)3, (CH2)5, etc.) II, III (R3 = R4 = H, Me) and IV bearing electrophile moieties were synthesized and biol. evaluated. The representative analog I (R1R2 = (CH2)3) exhibited potent anti-proliferative effect in MCF-7 cell lines in vitro, and further mechanism studies confirmed the necessity of covalent bonding. More importantly, I could attenuate the expression of TFF-1, GREB-1 and down-regulate the levels of cellular ERα protein. This study involved multiple reactions and reactants, such as 4-Benzyloxyphenol (cas: 103-16-2Recommanded Product: 4-Benzyloxyphenol).
4-Benzyloxyphenol (cas: 103-16-2) belongs to ethers. Esters typically have a pleasant smell; those of low molecular weight are commonly used as fragrances and are found in essential oils and pheromones. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Recommanded Product: 4-Benzyloxyphenol
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem