Abstract
COLCHICINE, the main alkaloid of Colchicum autumnale, is well known for its action on the mitotic spindle, resulting in an arrest of mitosis in metaphase. The synthesis of derivatives of this compound is of interest for several reasons. Some were used to elucidate the chemical structure of colchicine. In addition, many of them were tested for their ability to inhibit the growth of tumours. Furthermore, such compounds made possible an analysis of relationships between structure and biological activity of the colchicine molecule. In earlier investigations of the relation between structure and activity it was demonstrated that compounds lacking the acetyl group on the side-chain may be equally as active as colchicine1,2. In addition, the methoxy group on the tropolone ring could be replaced by a free or substituted amino group without loss of biological activity3.
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SCHINDLER, R. Desacetylamino-colchicine : a Derivative of Colchicine with Increased Cytotoxic Activity in Mammalian Cell Cultures. Nature 196, 73–74 (1962). https://doi.org/10.1038/196073b0
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DOI: https://doi.org/10.1038/196073b0
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