Effects of arenastatin A and its synthetic analogs on microtubule assembly.
Inhibition of microtubule assembly by arenastatin A (1) and five synthetic analogs (3-7) was examined. Arenastatin A and the triamide 6 showed potent and moderately strong inhibitory activities, respectively (IC50; 2.3 microM for 1, 7.8 microM for 6) and also depolymerized preformed microtubules. The other analogs tested showed no activity.
Koiso
Y
Y
Institute of Molecular and Cellular Biosciences, University of Tokyo, Japan.
Morita
K
K
Kobayashi
M
M
Wang
W
W
Ohyabu
N
N
Iwasaki
S
S
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001704:Biopolymers; D002455:Cell Division / Q000187:drug effects; D047630:Depsipeptides; D006801:Humans; D007624:KB Cells; D008854:Microscopy, Electron; D008870:Microtubules / Q000187:drug effects* / Q000648:ultrastructure; D010456:Peptides, Cyclic / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013552:Swine; D014404:Tubulin / Q000378:metabolism*
D000970:Antineoplastic Agents; D001704:Biopolymers; D047630:Depsipeptides; D010456:Peptides, Cyclic; D014404:Tubulin; C096566:arenastatin A