通过Biotage Isolera快速纯化液相制备色谱帮助进行新型的口服药紫杉烷类化合物的合成by耐士科技
2015-02-12 17:37
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A group of novel taxoids, with modifications at C-7, C-10, C-30 and C-14 positions of paclitaxel, was synthesized in order to improve their biological profile by decreasing their affinity with P-glycoprotein (Pgp) and increasing cellular permeability. Most of the new taxoids demonstrated the similar potent cytotoxic activities in MCF-7 human tumor cell line as paclitaxel in vitro. In the permeability assay with monolayers of Caco-2 cells, most of the compounds demonstrated an increased trans-cellular transport in Ato-
B direction in comparison with paclitaxel. Among them the compounds T-13, T-15 and T-26 showed the highest permeability, and with efflux ratios better than that of ortataxel. The interaction of the compounds T-13 and T-26 with P-gp was evaluated using Madin-Darby canine kidney (MDCK)-multidrug resistance-1(MDR1) and MDCK-wild-type (WT). The results indicated that T-13 and T-26 were poor substrates for P-gp and possessed inhibiting effects of P-gp mediated efflux. It was thus clear that simultaneous modifications at the C-7, C-10 and C-30 positions of paclitaxel significantly impaired its interactions with P-gp and interfered with P-gp mediated efflux.
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通过iotagesolera快速纯化液相制备色谱帮助进行新型的口服药紫杉烷类化合物的合成by耐士科技.pdf
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We herein report several highly active catalyst systems with thiadiazolidine 1-oxides as ligands for palladium in the MizorokieHeck reaction. Excellent yields of stilbenes derived from aryl iodides and bromides have been achieved using as little as 0.00002 mol % catalyst. The ligand/palladiumsystem can be stored as a stock solution open to air at room temperature with no observable loss of activity for a period of several months.
耐士科技作为Biotage中国区总代理,以优质的服务为您提供Biotage全系产品以及相关的技术服务。1、开机前确认自动收集机械手臂下无障碍物,试管高度低于机械手臂收集针
2、运行前确认所用流动相充足,废液瓶剩余空间充足
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1.开机,按屏幕左下方黑色电源键
2.进入开机界面后,点击Chemistry进入操作界面
3.在”Method”页面中设定好相关参数
耐士科技作为Biotage中国区总代理,以优质的服务为您提供Biotage全系产品以及相关的技术服务。
操作步骤:
1.开机,按屏幕左下方黑色电源键
2.进入开机界面后,点击
Organic Synthesis
进入编辑界面