Drugs, response alkaloids

Vinflumine (Javlor ) is a second-generation Vinca alkaloid. It is more active than the nonfluorinated parent compound (vinorelbine) in several cancers (Figure 8.7). Vinflumine is currently in Phase III clinical trials as a chemotherapeutic agent against a variety of cancers (metastasic breast cancer, small cell lung cancer, and bladder cancer). This drug inhibits mitotic assembly, via inhibition of tubulin polymerization in microtubules, a major element of the cytoskeleton. Effects of fluorine substimtion on tubulin affinity or on metabolism are not responsible for the increased efficiency and decreased toxicity. The synthesis of vinflumine is reported in Chapter 4. ... 

The beginning of alkaloid chemistry is usually considered to be 1805 when F.W. Sertiirner first isolated morphine. He prepared several salts of morphine and demonstrated that it was the principle responsible for the physiological effect of opium, Alkaloid research has continued to date, blit because most likely plant sources have been investigated and because a large number of synthebc drugs serve medical and other needs more effectively, the greatest emphasis has been placed upon the synthetics. 

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