Synthesis of Mustard-Derived and Heteroaromatic Combretastatin Analogues(superscript #)

The aim of this study was to delicately synthesize certain hybrid molecules bearing the mustard-derived and/or heterocyclic combretastain analogues to exploit new antitumor agents. Thus, a variety of heteroaromatic combretastatin analogues 8a-e were efficiently prepared and readily accessed to nitrogen mustard through an ester linkage. However, these delicately hybrid compounds were only shown moderate growth inhibitory potency with most IC50s at micromolar levels, which were much less potent than the natural CA-4 against the KB cells.