Synthesis and biological evaluation of aryl azide derivatives of combretastatin A-4 as molecular probes for tubulin

…, BE Rosenquist, GR Pettit, P Verdier-Pinard…

Index: Pinney, Kevin G.; Mejia, Maria P.; Villalobos, Victor M.; Rosenquist, Brent E.; Pettit, George R.; Verdier-Pinard, Pascal; Hamel, Ernest Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 10 p. 2417 - 2425

Full Text: HTML

Citation Number: 83

Abstract

Two new aryl azides,(Z)-1-(3′-azido-4′-methoxyphenyl)-2-(3 ″, 4 ″, 5 ″- trimethoxyphenyl) ethene 9 and (Z)-1-(4′-azido-3′-methoxyphenyl)-2-(3 ″, 4 ″, 5 ″- trimethoxyphenyl) ethene 5, modeled after the potent antitumor, antimitotic agent combretastatin A-4 (CA-4), have been prepared by chemical synthesis as potentially useful photoaffinity labeling reagents for the colchicine site on β-tubulin. Aryl azide 9, in which ...