Abstract
Analogs of hemiasterlin ( 1) and HTI-286 ( 2), which contain various aromatic rings in the A segment, were synthesized as potential inhibitors of tubulin polymerization. The structure–activity relationships related to stereo- and regio-chemical effects of substituents on the aromatic ring in the A segment were studied. Analogs, which carry a meta-substituted phenyl ring in the A segment show comparable activity for inhibition of tubulin polymerization to 2, as well as in the cell proliferation assay using KB cells containing P-glycoprotein, compared to those of 1 and 2.
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