Author/Authors :
Ayako Yamashita، نويسنده , , Emily B. Norton، نويسنده , , Joshua A. Kaplan، نويسنده , , Chuan Niu، نويسنده , , Frank Loganzo، نويسنده , , Richard Hernandez، نويسنده , , Carl F. Beyer، نويسنده , , Tami Annable، نويسنده , , Sylvia Musto، نويسنده , , Carolyn Discafani، نويسنده , , Arie Zask، نويسنده , , Semiramis Ayral-Kaloustian، نويسنده ,
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.
