The synthesis of amino-acid functionalized beta-carbolines as topoisomerase II inhibitors.
The synthesis and biological activity of amino acid functionalized beta-carboline derivatives, which are structurally related to azatoxin and the tryprostatins, are reported. These compounds were assayed for their growth inhibition properties in H520 and PC3 cell lines and were examined for their abilities to inhibit topoisomerase II-mediated DNA relaxation.
Deveau
A M
AM
Department of Chemistry, University of Virginia, Charlottesville 22901, USA.
Labroli
M A
MA
Dieckhaus
C M
CM
Barthen
M T
MT
Smith
K S
KS
Macdonald
T L
TL
D000596:Amino Acids / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002243:Carbolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors; D014407:Tumor Cells, Cultured / Q000187:drug effects / Q000201:enzymology
D000596:Amino Acids; D000970:Antineoplastic Agents; D002243:Carbolines; D004791:Enzyme Inhibitors; D059005:Topoisomerase II Inhibitors