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Natural Products pp 169–196Cite as

Case Studies in Natural-Product Optimization

Novel Antitumor Agents Derived From Taxus brevifolia and Catharanthus roseus

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Abstract

Taxus brevifolia is a Pacific yew tree that produces Taxol. Catharanthus roseus is one of the most well-studied plants in the world, and has provided 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. They are the most renowned natural products, have been successfully brought to market, and have also served as leads for further optimization. This review highlights the chemical modification of Taxus diterpenoids and bisindole Catharanthus alkaloids, with an emphasis on structure-activity relationship studies and analog optimizations, leading to the discovery of a new generation of antitumor drugs.

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  1. Discovery Chemistry Research & Technology, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN

    Jian Hong & Shu-Hui Chen

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  1. Jian Hong
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  1. Guangzhou Institute of Biomedicine and Health, Chinese Academy of Sciences, Guangzhou, China

    Lixin Zhang PhD

  2. SynerZ Pharmaceuticals Inc., Lexington, MA

    Lixin Zhang PhD

  3. Charles A. Dana Research Institute (R.I.S.E.), Drew University, Madison, NJ

    Arnold L. Demain PhD

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Hong, J., Chen, SH. (2005). Case Studies in Natural-Product Optimization. In: Zhang, L., Demain, A.L. (eds) Natural Products. Humana Press. https://doi.org/10.1007/978-1-59259-976-9_8

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