title: Total synthesis and biological evaluation of fluorinated cryptophycins.
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(50) 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.
authors.affiliation: Organic and Bioorganic Chemistry, Department of Chemistry, Bielefeld University, PO Box 100131, 33501 Bielefeld, Germany.
authors.forename: Christine
authors.initials: C
authors.lastname: Weiß
authors.forename: Tobias
authors.initials: T
authors.lastname: Bogner
authors.forename: Benedikt
authors.initials: B
authors.lastname: Sammet
authors.forename: Norbert
authors.initials: N
authors.lastname: Sewald