58750-86-0Relevant academic research and scientific papers
Discovery of N-(4-(Benzyloxy)-phenyl)-sulfonamide Derivatives as Novel Antagonists of the Human Androgen Receptor Targeting the Activation Function 2
Chai, Xin,Chen, Changwei,Cui, Sunliang,Fu, Yaqin,He, Junzhao,Hou, Tingjun,Li, Dan,Pang, Jinping,Shan, Luhu,Sun, Huiyong,Wang, Xinyue,Xu, Lei,Xu, Xiaohong,Yang, Liu,Yang, Yuhui,Yao, Xiaojun,Zhou, Wenfang
, p. 2507 - 2521 (2022/02/10)
Androgen receptor (AR) antagonists have been widely used for the treatment of prostate cancer (PCa). As a link between the AR and its transcriptional function, the activation function 2 (AF2) region has recently been revealed as a novel targeting site for developing AR antagonists. Here, we reported a series of N-(4-(benzyloxy)-phenyl)-sulfonamide derivatives as new-scaffold AR antagonists targeting the AR AF2. Therein, compound T1-12 showed excellent AR antagonistic activity (IC50 = 0.47 μM) and peptide displacement activity (IC50 = 18.05 μM). Furthermore, the in vivo LNCaP xenograft study confirmed that T1-12 offered effective inhibition on tumor growth when administered intratumorally. The study represents the first successful attempt to identify a small molecule targeting the AR AF2 with submicromolar AR antagonistic activity by structure-based virtual screening and provides important clues for the development of novel therapeutics for PCa treatment.
Methylprenyl and prenyl protection for sulfonamides
Nikitjuka, Anna,Nekrasova, Aleksandra,Jirgensons, Aigars
supporting information, p. 183 - 186 (2015/03/04)
2-Methylprenyl (MePre) is an efficient protection for sulfonamides. The acidic cleavage of this group leads to volatile by-products and the product can be obtained in high purity without additional purification. MePre group is resistant to Pd/C-catalysed hydrogenolysis at 1 atm, Suzuki-Miyaura reaction, Ni(0) catalysis conditions and oxidising reagents such as NIS and DDQ. The prenyl (Pre) group can also be used to protect sulfonamides in certain cases; however, the substrate scope is limited due to the side product formation.
Methylprenyl and prenyl protection for sulfonamides
Nikitjuka, Anna,Nekrasova, Aleksandra,Jirgensons, Aigars
supporting information, (2015/02/02)
2-Methylprenyl (MePre) is an efficient protection for sulfonamides. The acidic cleavage of this group leads to volatile by-products and the product can be obtained in high purity without additional purification. MePre group is resistant to Pd/C-catalysed hydrogenolysis at 1 atm, Suzuki-Miyaura reaction, Ni(0) catalysis conditions and oxidising reagents such as NIS and DDQ. The prenyl (Pre) group can also be used to protect sulfonamides in certain cases; however, the substrate scope is limited due to the side product formation.
