小檗碱类生物碱的部分合成及其抗微管蛋白活性：N-乙酰乙酰基去乙酰秋水仙碱和2-去甲基speciosine（speciocolchine）。

Partial synthesis and antitubulin activity of minor colchicum alkaloids: N-acetoacetyl-deacetylcolchicine and 2-demethylspeciosine (speciocolchine).

作者信息

Muzaffar A, Brossi A, Hamel E

机构信息

Section on Natural Products, Laboratory of Structural Biology, NIDDK, Bethesda, Maryland 20892.

出版信息

J Nat Prod. 1990 Jul-Aug;53(4):1021-4. doi: 10.1021/np50070a044.

DOI:10.1021/np50070a044

PMID:2095370

Abstract

Two minor Colchicum alkaloids, N-acetoacetyl-deacetylcolchicine [1] and 2-demethylspeciosine [7], were synthesized. The diacetate 8 of 2-demethylspeciosine was also prepared. The antitubulin activity of these compounds, in comparison to colchicine, was measured. N-Acetoacetyl-deacetylcolchicine [1] has in vitro activity similar to that of colchicine. Both 2-demethylspeciosine [7] and the diacetate 8 were considerably less potent inhibitors of tubulin polymerization.

摘要

合成了两种小檗碱生物碱，即N-乙酰乙酰基去乙酰秋水仙碱[1]和2-去甲基speciosine[7]。还制备了2-去甲基speciosine的二乙酸酯8。测定了这些化合物与秋水仙碱相比的抗微管蛋白活性。N-乙酰乙酰基去乙酰秋水仙碱[1]具有与秋水仙碱相似的体外活性。2-去甲基speciosine[7]和二乙酸酯8对微管蛋白聚合的抑制作用都要弱得多。