54313-35-8Relevant articles and documents
Design, synthesis of a novel 4-O-methylsaucerneol analogue LXY7824 as potent HIF-1 inhibitor and anti-cancer agent
Liu, Xiao-Yu,Li, Xiao-Yu,Yang, Fei-Long,Li, Yan,Jiao, Xiao-Zhen,Xie, Ping
, p. 545 - 558 (2018)
Hypoxia-inducible factor-1 (HIF-1), an important transcription factor for tumor survival, is an attractive target for anti-cancer treatment. Herein, we present the design and synthesis of LXY7824, a simplified analogue of 4-O-methylsaucerneol. In addition
Facile and Divergent Synthesis of Lamellarins and Lactam-Containing Derivatives with Improved Drug Likeness and Biological Activities
Theppawong, Atiruj,Ploypradith, Poonsakdi,Chuawong, Pitak,Ruchirawat, Somsak,Chittchang, Montakarn
, p. 2631 - 2650 (2016/02/09)
With the goal to improve the aqueous solubility of lamellarins, the lactone ring in their skeleton was replaced with a lactam moiety in azalamellarins. However, the reported synthetic route produced such derivatives in very low yields. Hence, this study focused on developing an efficient simplified total synthetic scheme that could furnish both azalamellarins and the parent lamellarins from the same pyrrole ester intermediates. Subsequent comparative profiling revealed that the introduced lactone-to-lactam replacement rendered these molecules less lipophilic, whereas their cancer cytotoxicity remained equipotent to that of the parent compounds. Interestingly, their inhibitory activity was significantly enhanced towards the multifaceted GSK-3β enzyme. Our results clearly demonstrate the therapeutic potential of this promising class of marine-derived natural products and justify their further development, especially into anticancer agents.
First enantioselective syntheses of the dopamine D1 and D2 receptor modulators, (+)-and (-)-govadine
Zhai, Huimin,Miller, James,Sammis, Glenn
scheme or table, p. 1557 - 1559 (2012/04/04)
There is a pressing need to find and develop new antipsychotic agents for the treatment of schizophrenia. Current drugs primarily target dopamine D2receptors and are only effective in the treatment of the positive symptoms of this indication. The tetrahyd