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Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids
Shiqing Han1, Ernest Hamel, Kenneth F Bastow
1Natural Products Laboratory, School of Pharmacy, University of North Carolina at Chapel Hill, NC 27599, USA.
Bioorganic & Medicinal Chemistry Letters
|September 25, 2002
Abstract:
N-Acetylcolchinol methyl ether 1 served as the starting material to prepare the chloroacetamide (3) and epoxide (5) analogues. Both 3 and 5 were potent inhibitors of tubulin polymerization in vitro. Compound 3 was also 4-fold more cytotoxic than colchicine against the 1A9 tumor cell line and showed a unique cross-resistance profile.