Frontiers in Natural Product Chemistry

Volume: 1

Synthesis of Vinblastine Derivatives

Author(s): Hedvig Bolcskei, Lajos Szabo and Csaba Szantay

Pp: 43-49 (7)

DOI: 10.2174/978160805212710501010043

* (Excluding Mailing and Handling)


The bisindole alkaloids of the Madagascan periwinkle Catharanthus Roseus vincristine 1 and vinblastine 2 are widely used clinically in the chemotherapy of cancer. Many efforts were made to synthesize more efficient new derivatives having less side effects than vinblastine 2. New anhydrovinblastine derivatives were obtained by the ferric chloride mediated coupling reaction of catharanthine and vindoline and their derivatives. The nitro- dinitro-, amino- and hydroxymethyl analogues of the alkaloids 1, 2 and 3 showed promising antitumor activity.

Keywords: catharanthus roseus, vincristine, antineoplastic agents, chemotherapy, indole alkaloids, nmr study

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