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Heterocyclic Antitumor Antibiotics pp 1–51Cite as

Synthesis of Biologically Active Heterocyclic Stilbene and Chalcone Analogs of Combretastatin

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Part of the book series: Topics in Heterocyclic Chemistry ((TOPICS,volume 2))

Abstract

Combretastatin A-4 (CA-4, 7) has had a major impact in the field of medicinal chemistry as a potent bioactive molecule that binds to the cholchicine site of tubulin. However, its poor water solubility spurred a wealth of research into analogs to overcome these pharmakokinetic deficiencies. The focus of this chapter is the recent synthesis of novel and interesting biologically active heterocyclic analogs of CA-4, 7 that possess the stilbene and chalcone core. This review will also discuss alternative methods of synthesizing potentially biologically active derivatives of CA-4, 7, reported in the last 5 years.

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Author information

Authors and Affiliations

  1. Department of Chemistry, Hope College, 49423, Holland, MI, USA

    Toni Brown

  2. Department of Chemistry, University of North Carolina, 28804, Asheville, NC, USA

    Herman Holt Jr.

  3. Dean of Natural Sciences, Hope College, 49423, Holland, MI, USA

    Moses Lee

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  1. Toni Brown
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  2. Herman Holt Jr.
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  3. Moses Lee
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Correspondence to Moses Lee .

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Moses Lee

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Brown, T., Holt Jr., H., Lee, M. Synthesis of Biologically Active Heterocyclic Stilbene and Chalcone Analogs of Combretastatin. In: Lee, M. (eds) Heterocyclic Antitumor Antibiotics. Topics in Heterocyclic Chemistry, vol 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/7081_003

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