1451207-88-7Relevant articles and documents
Rearrangement of 2-bromo-1-(bromomethyl)ethyl esters under basic conditions: Scope and mechanism
Alliot, Julien,Gravel, Edmond,Doris, Eric
, p. 2861 - 2866 (2013)
A novel rearrangement of 2-bromo-1-(bromomethyl)ethyl esters into the corresponding 2-oxopropyl derivatives is reported. The mechanism of this transformation was studied by means of 18O- and 2H- labeling experiments. The reaction pro
The first synthesis of natural disulfide bruguiesulfurol and biological evaluation of its derivatives as a novel scaffold for PTP1B inhibitors
Chen, Jing,Jiang, Cheng-Shi,Ma, Wen-Quan,Gao, Li-Xin,Gong, Jing-Xu,Li, Jing-Ya,Li, Jia,Guo, Yue-Wei
, p. 5061 - 5065 (2013/09/12)
Bruguiesulfurol (1), a cyclic 4-hydroxy-dithiosulfonate isolated from mangrove plant Bruguiera gymnorrhiza, was concisely synthesized for the first time in four steps, and a series of its synthetic derivatives were evaluated for in vitro inhibitory effects on PTP1B and related PTPs. Some derivatives were found to have improved pharmacological profile compared with hit 1. Among them, 5a showed the potent selectivity towards PTP1B over other PTPs, including TCPTP, and 7j exhibited the strongest PTP1B inhibitory activity with an IC 50 value of 4.54 μM.