1060689-22-6Relevant articles and documents
Discovery of novel taspine derivatives as antiangiogenic agents
Zhang, Jie,Zhang, Yanmin,Zhang, Sanqi,Wang, Sicen,He, Langchong
scheme or table, p. 718 - 721 (2010/05/18)
VEGFR-2 plays a critical role in vasculogenesis and inhibitors of VEGFR-2 could be used in the treatment of cancer. Taspine was one of the active ingredients screened by using an endothelial cell membrane chromatography and showed inhibition against VEGFR-2. In our research, we explored how the lactone ring and biphenyl scaffold in taspine influence its potent in vitro anticancer and antiangiogenesis activities. Accordingly, we report the design, synthesis, and preliminary evaluation of four novel taspine derivatives as VEGFR-2 inhibitors. The preliminary biological test showed that one of the compounds showed much better inhibitory activities against CACO-2 (IC50 = 52.5 nM) and ECV304 (IC50 = 2.67 nM) than taspine. This result enlarges the interest in ring-opened taspine derivative skeleton in the search of new antiangiogenesis agents.
Efficient synthesis of thalifoline and its analogs
Li, Qiang,Zhang, San-Qi,Wang, Si-Cen,Zhou, Ming-Zhe
experimental part, p. 1752 - 1758 (2009/10/06)
Thalifoline (1) and its analogs were synthesized from methyl 3-hydroxy-4-methoxy benzoate by prenyl etherification, Claisen rearrangement, oxidation, imine formation, reductive amination and intramolecular amidation. The last three steps, imine formation,
