The synthesis and evaluation of benzannelated-azatoxins: the benzazatoxins.
The synthesis and evaluation of azatoxin congeners possessing annealed aromatic frameworks are described. The compounds were evaluated for their abilities to affect topoisomerase II inhibition through the stabilization of "cleavable complex" and for the inhibition of tubulin polymerization using purified bovine brain tubulin.
Miller
T A
TA
Department of Chemistry, University of Virginia, Charlottesville 22902, USA.
Vachaspati
P R
PR
Labroli
M A
MA
Thompson
C D
CD
Bulman
A L
AL
Macdonald
T L
TL
D000818:Animals; D001921:Brain / Q000378:metabolism; D002417:Cattle; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007202:Indicators and Reagents; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007700:Kinetics; D008968:Molecular Conformation; D015394:Molecular Structure; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors; D014404:Tubulin / Q000187:drug effects
D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D007211:Indoles; D011810:Quinoxalines; D059005:Topoisomerase II Inhibitors; D014404:Tubulin; C075996:azatoxin