Current Efforts Towards the Preparation of 2'-Aminotaxol
As the most promising anticancer drug TaxolŽ has been the subject of intense research for almost four decades. SAR studies showed that the presence of 2'-hydroxyl group is crucial for good bioactivity and is believed to be due to its hydrogen bonding capacity. Two different hypotheses exist: One stipulates that a hydrogen bond is formed between the 2'-hydroxyl and 1'-carbonyl groups that fixes the flexible side chain in its active conformation; the other proposes that the 2'-hydroxyl group interacts directly with residues at the microtubule binding site. To investigate these two different hypotheses the synthesis of a 2'-amino derivative is being attempted. This poster presents the current status of the project.
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