Synthesis and evaluation of double bond substituted combretastatins

Hadfield, JA; Gaukroger, K; Hirst, N; Weston, AP; Lawrence, NJ; McGown, AT

Abstract

A series of combretastatins substituted with epoxides, amides and small alkyl groups has been synthesised and evaluated for cytotoxicity and their ability to inhibit the assembly of tubulin. The methyl and ethyl substituted phenols 36, 44 have shown potent antimitotic effects whilst exhibiting reduced cytotoxicity.

Citation

Hadfield, J., Gaukroger, K., Hirst, N., Weston, A., Lawrence, N., & McGown, A. (2005). Synthesis and evaluation of double bond substituted combretastatins. European Journal of Medicinal Chemistry, 40(6), 529-541. https://doi.org/10.1016/j.ejmech.2004.12.008

• Journal Article Type: Article
• Publication Date: Apr 1, 2005
• Deposit Date: Aug 7, 2007
• Journal: European Journal of Medicinal Chemistry
• Print ISSN: 0223-5234
• Publisher: Elsevier
• Peer Reviewed: Peer Reviewed
• Volume: 40
• Issue: 6
• Pages: 529-541
• DOI: https://doi.org/10.1016/j.ejmech.2004.12.008
• Keywords: Combretastatin; Tubulin; Antimitotic
• Publisher URL: http://www.sciencedirect.com/science?_ob=ArticleURL&_udi=B6VKY-4FNDRVY-2&_user=899537&_coverDate=06%2F30%2F2005&_rdoc=3&_fmt=high&_orig=browse&_srch=doc-info(%23toc%236135%232005%23999599993%23597058%23FLA%23display%23Volume)&_cdi=6135&_sort=d&_docanchor=