化药新药研发其他>方法开发检测 | 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-上海鑫欣生物科技有限公司

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应用领域	制药/生物制药
检测样本	化药新药研发
检测项目	其他>方法开发
参考标准	GB/T 8****

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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上一篇耐士科技：使用Biotage Isolera快速纯化液相制备色谱从库拉索芦荟叶皮提取天然的磷酸二酯酶抑制剂by耐士科技

下一篇通过Biotage Isolera快速纯化液相制备色谱帮助使用仿生的直接环氧化反应和天然产物的结构重排进行ent-(-)-azonazine的全合成研究by耐士科技

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