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Total synthesis and biological evaluation of fluorinated cryptophycins

By Christine Wei&#223, Tobias Bogner, Benedikt Sammet and Norbert Sewald

Abstract

Cryptophycins are cytotoxic natural products that exhibit considerable activities even against multi-drug-resistant tumor cell lines. As fluorinated pharmaceuticals have become more and more important during the past decades, fluorine-functionalized cryptophycins were synthesized and evaluated in cell-based cytotoxicity assays. The unit A trifluoromethyl-modified cryptophycin proved to be highly active against KB-3-1 cells and exhibited an IC<sub>50</sub> value in the low picomolar range. However, the replacement of the 3-chloro-4-methoxyphenyl-substituent in unit B by a pentafluorophenyl moiety resulted in a significant loss of activity

Topics: antimitotic drug, cytotoxicity, depsipeptide, fluorinated natural product analogues, structure-activity relationship, Organic chemistry, QD241-441, Chemistry, QD1-999, Science, Q, DOAJ:Organic Chemistry, DOAJ:Chemistry
Publisher: Beilstein-Institut
Year: 2012
DOI identifier: 10.3762/bjoc.8.231
OAI identifier: oai:doaj.org/article:1a8ba266108d484ebff6e7de7ca2b820
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