Synthesis and biological evaluation of C-3'NH/C-10 and C-2/C-10 modified paclitaxel analogues |
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| Authors: | Baloglu Erkan Hoch Jeannine M Chatterjee Sabarni K Ravindra Rudravajhala Bane Susan Kingston David G I |
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| Institution: | Department of Chemistry, M/C 0212, Virginia Polytechnic Institute and State University, Blacksburg, VA 24061, USA. |
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| Abstract: | Concurrent modifications on the C-3'NH/C-10, and C-2/C-10 positions on paclitaxel were carried out as a way of investigating possible synergistic effects. The biological activities of these analogues were evaluated in both a microtubule assembly assay and human ovarian cancer (A2780) and prostate cancer (PC3) cytotoxicity assay. In some cases the doubly modified analogues were more active than would have been predicted based on the activity of the singly modified analogues, indicating probable synergistic effects. |
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