Synthesis and evaluation of 3D templates based on a taxane skeleton to circumvent P-glycoprotein-associated multidrug resistance of cancer

We have developed a practical synthetic route to construct C-aromatic taxane derivatives as three-dimension templates by way of intramolecular alkylation. The usefulness of synthesized compounds as the core template was evaluated by using a newly developed screening system for P-glycoprotein.

The synthesis of the C-aromatic taxoid analogues 1–3, and their affinity for P-glycoprotein are reported. An evolution of multidrug resistant reversal activity of 2b is also described.Figure optionsDownload as PowerPoint slide