کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1361743 | 981470 | 2011 | 5 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport Effects of C7 substitutions in a high affinity microtubule-binding taxane on antitumor activity and drug transport](/preview/png/1361743.png)
Some C-7 modified analogs of 3, a taxane with high affinity for binding to microtubules, were prepared through multistep transformations. Most of the analogs, bearing less lipophilic C-7 substituents than propionyl in 3, exhibited comparable binding affinities to microtubules but less cytotoxicity against drug-sensitive as well as multidrug-resistant tumor cells overexpressing P-glycoprotein. In addition, these C7 modifications increased P-glycoprotein-mediated drug transport in both directions in a Caco-2 cell assay.
Some C-7 modified analogs of 3, a taxane with high affinity for binding to microtubules were prepared. Most of the analogs, bearing less lipophilic C-7 substituents than propionyl in 3, exhibited comparable binding affinities to microtubules but less cytotoxicity against drug-sensitive and multidrug-resistant tumor cells overexpressing P-glycoprotein. In addition, these C7 modifications increased P-glycoprotein-mediated drug transport in both directions in a Caco-2 cell assay.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 16, 15 August 2011, Pages 4852–4856