کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1367388 | 981630 | 2006 | 5 صفحه PDF | دانلود رایگان |
In the present work, we explore the possibility of introducing selectivity to existing chemotherapeutics via the design of non-pro-drug, bi-functional molecules comprising a microtubule-binding agent and a substrate for a disease-associated kinase. The design, synthesis, and in vitro biological evaluation of paclitaxel–thymidine and vinblastine–thymidine bi-functional conjugates are reported here. This work provides the first account of ‘kinase-mediated trapping’ of cancer therapeutics.
In the present work, we explore the possibility of introducing selectivity to existing chemotherapeutics via the design of non-pro-drug, bi-functional molecules comprising a microtubule-binding agent and a substrate for a disease-associated kinase. The design, synthesis, and in vitro biological evaluation of paclitaxel–thymidine and vinblastine–thymidine bi-functional conjugates are reported here. This work provides the first account of ‘kinase-mediated trapping’ of cancer therapeutics.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 16, Issue 19, 1 October 2006, Pages 5194–5198