Conformationally restricted paclitaxel analogues: macrocyclic mimics of the "hydrophobic collapse" conformation.
Conformationally restricted macrocyclic analogues of paclitaxel were prepared, by connecting the 3'-phenyl group and the 2-benzoate moiety with two-atom tethers to mimic the "hydrophobic collapse" paclitaxel conformation. The analogues did not show activity in a tubulin assembly assay.
Boge
T C
TC
Department of Medicinal Chemistry, University of Kansas, Lawrence 66045, USA.
Wu
Z J
ZJ
Himes
R H
RH
Vander Velde
D G
DG
Georg
G I
GI
D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry*; D008968:Molecular Conformation; D017239:Paclitaxel / Q000737:chemistry*
D000972:Antineoplastic Agents, Phytogenic; D017239:Paclitaxel