1078733-91-1Relevant academic research and scientific papers
Rational design and optimization of selenophenes with basic side chains as novel potent selective estrogen receptor modulators (SERMs) for breast cancer therapy
Luo, Junjie,Hu, Zhiye,Xiao, Yuan,Yang, Tongxin,Dong, Chune,Huang, Jian,Zhou, Hai-Bing
, p. 1485 - 1497 (2017/07/25)
To increase the diversity of estrogen receptor (ER) ligands having novel structures and activities, series of selenophene derivatives with a basic side chain (BSC) were synthesized and their biological activity as subtype-selective antagonists for the ER was explored. Compared with the selenophenes without a BSC, most compounds showed an increase in binding affinity, and several compounds displayed enhanced antagonist potency and antiproliferative activity. Especially, compound 16c exhibited excellent transcriptional activity for ERα (IC50 = 13 nM) which made this compound the most potent antagonist for ERα of the whole series and is 66-fold better than the best selenophene compound without a BSC. Moreover, several compounds showed values of IC50 better than that of 4-hydroxytamoxifen in breast cancer MCF-7 cells. The modeling study indicated that the basic side chain might contribute to their increased antagonist potency and antiproliferative activity. These new ligands have the potential to be further developed as novel agents to improve therapeutics that target the estrogen receptor.
Selenophenes: Introducing a New Element into the Core of Non-Steroidal Estrogen Receptor Ligands
Zhang, Silong,Wang, Zhiyong,Hu, Zhiye,Li, Changhao,Tang, Chu,Carlson, Kathryn E.,Luo, Junjie,Dong, Chune,Katzenellenbogen, John A.,Huang, Jian,Zhou, Hai-Bing
, p. 235 - 249 (2017/02/15)
The importance of the heterocyclic core elements with peripheral phenolic and alkyl substituents as a dominant structural motif of ligands for the estrogen receptor (ER) has been well recognized. In this study we expanded the structural diversity of core
Selenophen compound
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Paragraph 0017, (2016/10/08)
The invention belongs to the technical field of medicines and in particular discloses a selenophen compound which takes an estrogen receptor as a target point, has resistance to hormone-dependent (positive ER+) breast cancer and also has high inhibitory a
Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1)
Bey, Emmanuel,Marchais-Oberwinkler, Sandrine,Werth, Ruth,Negri, Matthias,Al-Soud, Yaseen A.,Kruchten, Patricia,Oster, Alexander,Frotscher, Martin,Birk, Barbara,Hartmann, Rolf W.
experimental part, p. 6725 - 6739 (2009/11/30)
17β-Estradiol (E2), the most potent female sex hormone, stimulates the growth of mammary tumors and endometriosis via activation of the estrogen receptor α (ERα). 17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1), which is responsible for the catalytic r
