Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids |
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| Authors: | Han Shiqing Hamel Ernest Bastow Kenneth F McPhail Andrew T Brossi Arnold Lee Kuo-Hsiung |
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| Affiliation: | Natural Products Laboratory, School of Pharmacy, University of North Carolina at Chapel Hill, NC 27599, USA. |
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| 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. |
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