Going to trial: From about 350 active epothilone analogues synthesized by a highly convergent synthesis, one (ZK-EPO, see picture) has been chosen for clinical development on the basis of its outstanding preclinical data. This compound exhibits higher activity and efficacy than taxanes (e.g. paclitaxel) and second-generation epothilones, a fast and efficient cellular uptake, no recognition by efflux mechanisms, and an improved therapeutic window. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2006/z602785_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
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Klar et al. (2006) studied this question.
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