Abstract:
Vinblastine (VLB) and vincristine (VCR) are both being used in medical practice as drugs of choice in several malignant conditions. Vinblastine has been found specially useful in the treatment .of Hodgkins disease and choriocarcinoma while vincristine finds its main use in acute leukaemia in children. The structures of these binary alkaloids have been determined and confirmed by X-ray crystallography of vincristine methiodide. Although both vinblastine and vincristine are highly active, they occur only in minute traces in the leaves of Catharanthus roseus and their isolation involves a cumbersome procedure involving separation on the basis of their differential basicities followed by chromatography. Their availability on a commercial scale therefore poses a serious problem to the pharmaceutical industry and raises their cost to several thousand dollars per gram. Their synthesis has therefore attracted the attention of several eminent chemists over the last decade. All previous efforts have however been unsuccessful due to the complexity of the structures of these alkaloids. The first partial synthesis of both vinblastine and vincristine was reported by the writer and his co workers in 1976. The synthesis was based on a biosynthetic hypothesis which has subsequently been verified and has formed the basis of recent dramatic advances in the field of synthesis of these highly active anti-cancer drugs.
Page(s):
81-93
DOI:
DOI not available
Published:
Journal: Journal of Chemical Society of Pakistan, Volume: 1, Issue: 1, Year: 1979