1233720-57-4Relevant academic research and scientific papers
2-Phenylbenzo[b]furans: Synthesis and promoting activity on estrogen biosynthesis
Pu, Wenchen,Yuan, Yun,Lu, Danfeng,Wang, Xin,Liu, Hanwei,Wang, Chun,Wang, Fei,Zhang, Guolin
, p. 5497 - 5500 (2016/11/09)
Estrogen biosynthesis is pivotal to many physiological processes of human. Aberrant estrogen level is closely related to a variety of diseases, including breast cancer and osteoporosis. Previously we found that 2-phenylbenzo[b]furan glycosides could promote estrogen biosynthesis. To find high active 2-phenylbenzo[b]furans, fifty-four 2-phenylbenzo[b]furans were prepared via four strategies according to corresponding substrate scopes. Biological evaluation in HEK293A cells showed that some compounds exhibited promotive activity on estrogen biosynthesis. 2-(4-Chlorophenyl)-7-methoxybenzo[b]furan possessed the highest activity with EC50value of 14.68?μM. Furthermore, these compounds did not affect aromatase expression in HEK292A cells, indicating that these 2-phenylbenzo[b]furans might enhance estrogen biosynthesis via directly allosteric regulation of aromatase or indirectly via posttranslational modification.
Total synthesis of ailanthoidol, egonol, and related analogues
Duan, Xin-Fang,Shen, Gang,Zhang, Zhan-Bin
experimental part, p. 1181 - 1187 (2010/06/12)
Efficient and general synthetic protocols were developed for the total synthesis of ailanthoidol, egonol, and some related analogues. The key transformations describe here involve a two-step construction of the benzofuran and a Sonogashira coupling, and proved to be convenient and effective, starting from readily available reagents.
A concise synthesis of natural benzofuran neolignans and analogues
Duan, Xin-Fang,Shen, Gang,Zhang, Zhan-Bin
experimental part, p. 2547 - 2552 (2010/09/08)
The first total synthesis of four naturally occurring benzofuran neolignans and two analogues was achieved in four steps in 44-51% overall yield. Key steps involved a two-step construction of benzofuran nucleus and a Suzuki coupling. This synthesis has been proven straightforward and efficient, and more related analogues can be prepared for structure-activity relationship explorations. Georg Thieme Verlag Stuttgart New York.
