Design and Synthesis of Basic Selective Estrogen Receptor Degraders for Endocrine Therapy Resistant Breast Cancer was written by Lu, Yunlong;Gutgesell, Lauren M.;Xiong, Rui;Zhao, Jiong;Li, Yangfeng;Rosales, Carlo I.;Hollas, Michael;Shen, Zhengnan;Gordon-Blake, Jesse;Dye, Katherine;Wang, Yueting;Lee, Sue;Chen, Hu;He, Donghong;Dubrovyskyii, Oleksii;Zhao, Huiping;Huang, Fei;Lasek, Amy W.;Tonetti, Debra A.;Thatcher, Gregory R. J.. And the article was included in Journal of Medicinal Chemistry in 2019.Application In Synthesis of 4-Benzyloxyphenol The following contents are mentioned in the article:
The clin. steroidal selective estrogen receptor (ER) degrader (SERD), fulvestrant, is effective in metastatic breast cancer, but limited by poor pharmacokinetics, prompting the development of orally bioavailable, nonsteroidal SERDs, currently in clin. trials. These trials address local breast cancer as well as peripheral metastases, but patients with brain metastases are generally excluded because of the lack of blood-brain barrier penetration. A novel family of benzothiophene SERDs with a basic amino side arm (B-SERDs) was synthesized. Proteasomal degradation of ERα was induced by B-SERDs that achieved the objectives of oral and brain bioavailability, while maintaining high affinity binding to ERα and both potency and efficacy comparable to fulvestrant in cell lines resistant to endocrine therapy or bearing ESR1 mutations. A novel 3-oxyazetidine side chain was designed, leading to 37d, a B-SERD that caused endocrine-resistant ER+ tumors to regress in a mouse orthotopic xenograft model. This study involved multiple reactions and reactants, such as 4-Benzyloxyphenol (cas: 103-16-2Application In Synthesis of 4-Benzyloxyphenol).
4-Benzyloxyphenol (cas: 103-16-2) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Because of their lack of hydrogen-bond-donating ability, esters do not self-associate. Consequently, esters are more volatile than carboxylic acids of similar molecular weight.Application In Synthesis of 4-Benzyloxyphenol
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem