Abstract
Taxus brevifolia is the pacific yew tree from which paclitaxel (Taxol®) was first isolated. Catharanthus roseus, one of the most extensively studied medicinal plants in the world, has provided modern pharmacology with a large number of alkaloids, including the clinically important antitumor agents vinblastine and vincristine. Both classes of antitumor agents interfere with tubulin-microtubule dynamics through opposite modes of action. Considered to be excellent natural products, these drugs have been successfully brought to the market and served as leads for further optimization. This review highlights the chemical modification of Taxus diterpenoids and bisindole Catharanthus alkaloids, with emphasis on structure-activity relationship (SAR) studies and analogue optimization, which have culminated in the discovery of a new generation of antitumor drugs.
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