36722-81-3Relevant academic research and scientific papers
Synthesis and biological evaluation of new carbohydrate-substituted indenoisoquinoline topoisomerase I inhibitors and improved syntheses of the experimental anticancer agents indotecan (LMP400) and indimitecan (LMP776)
Beck, Daniel E.,Agama, Keli,Marchand, Christophe,Chergui, Adel,Pommier, Yves,Cushman, Mark
, p. 1495 - 1512 (2014/03/21)
Carbohydrate moieties were strategically transported from the indolocarbazole topoisomerase I (Top1) inhibitor class to the indenoisoquinoline system in search of structurally novel and potent Top1 inhibitors. The syntheses and biological evaluation of 20 new indenoisoquinolines glycosylated with linear and cyclic sugar moieties are reported. Aromatic ring substitution with 2,3-dimethoxy-8,9-methylenedioxy or 3-nitro groups exerted strong effects on antiproliferative and Top1 inhibitory activities. While the length of the carbohydrate side chain clearly correlated with antiproliferative activity, the relationship between stereochemistry and biological activity was less clearly defined. Twelve of the new indenoisoquinolines exhibit Top1 inhibitory activity equal to or better than that of camptothecin. An advanced synthetic intermediate from this study was also used to efficiently prepare indotecan (LMP400) and indimitecan (LMP776), two anticancer agents currently under investigation in a Phase I clinical trial at the National Institutes of Health.
Antioxidant activity of a water-soluble polysaccharide purified from Pteridium aquilinum
Xu, Wentao,Zhang, Fangfang,Luo, YunBo,Ma, Liyan,Kou, Xiaohong,Huang, Kunlun
experimental part, p. 217 - 222 (2009/04/11)
A water-soluble crude polysaccharide, obtained from fern Pteridium aquilinum, was fractionated by DEAE-Sepharose Fast-Flow column chromatography, and purified by Sephacryl S-400 HR column chromatography. The average molecular weight (Mw) of the purified polysaccharide (PLP) is 458,000 Da. The monosaccharide components of PLP were characterized by gas chromatography (GC), and the majority of the monosaccharide components was glucose (relative mass 58.1%) with low levels of galactose, mannose, rhamnose, and arabinose (relative mass 18.7%, 6.8%, 10.2%, and 6.1%, respectively). The Fourier-transform infrared spectra (FTIR) of PLP revealed typical characteristics of polysaccharides. On the basis of the ferric-reducing antioxidant power assay (FRAP), DPPH radical-scavenging, the superoxide radical assay, and self-oxidation of 1,2,3-phentriol assay, the antioxidant activities of PLP were investigated. The purified polysaccharide was demonstrated to have strong reductive power (FRAP value: 827.6 μmol/L), moderate scavenging activities against DPPH radicals (83.1%) and superoxide radicals (60.5%), and moderate inhibiting power for self-oxidation of 1,2,3-phentriol (52.4%).
