Abstract
The synthetic investigation of biologically active natural compounds serves two main purposes: (i) the total synthesis of alkaloids and their analogues; (ii) modification of the structures for producing more selective, more effective, or less toxic derivatives. In the chemistry of dimeric Vinca alkaloids enormous efforts have been directed towards synthesizing new derivatives of the antitumor agents vinblastine and vincristine so as to obtain novel compounds with improved therapeutic properties.
Highlights
Vinblastine (1) and vincristine (2) are dimeric alkaloids (Figure 1) isolated from the Madagaskar periwinkle plant (Catharantus roseus), exhibit significant cytotoxic activity and are used in the antitumor therapy as antineoplastic agents.In the course of cell proliferation they act as inhibitors during the metaphase of the cell cycle and by binding to the microtubules inhibit the development of the mitotic spindle
Numerous derivatives of vinblastine and vincristine were prepared by Boger [39]
One of the examples is the synthesis of carbamates of vindoline in position 16 (Scheme 30) and after coupling with catharanthine (3) new derivatives 80 and 81 of vinblastine were obtained which had important anticancer activity against human non-small cell lung cancer and on human cervix epithelial adenocarcinoma cell lines [44]
Summary
Vinblastine (1) and vincristine (2) are dimeric alkaloids (Figure 1) isolated from the Madagaskar periwinkle plant (Catharantus roseus), exhibit significant cytotoxic activity and are used in the antitumor therapy as antineoplastic agents. In the course of cell proliferation they act as inhibitors during the metaphase of the cell cycle and by binding to the microtubules inhibit the development of the mitotic spindle. In tumor cells these agents inhibit the DNA repair and the RNA synthesis mechanisms, blocking the DNA-dependent. The aim of our present work, is to highlight the different derivatives and derivatisations of vinblastine (1) and vincristine (2), focusing primarily on selected cases that stand out from the enormous literature data owing to their interesting chemistry or important biological effects
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