Rigid Analogs of Camptothecin as DNA Topoisomerase I Inhibitors

Substituted 8-ethyl-2-(2-oxo-1,2-dihydroindol-3-ylidene)-8-hydroxy-2,3,5,8- tetrahydro-6-oxa-3a-azacyclopenta[b]naphthalene-1,4,7-triones were synthesized and evaluated as topoisomerase I inhibitors in an in vitro cleavable complex assay. The activity of these compounds may be attributed to their ri...

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Veröffentlicht in:	Journal of medicinal chemistry 1995-03, Vol.38 (6), p.906-911
Hauptverfasser:	Lackey, Karen, Besterman, Jeffrey M, Fletcher, Wade, Leitner, Peter, Morton, Bradley, Sternbach, Daniel D
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkaloids - chemical synthesis Alkaloids - pharmacology Analytical, structural and metabolic biochemistry Antineoplastic Agents - chemical synthesis Antineoplastic Agents - pharmacology Biological and medical sciences Camptothecin - analogs & derivatives DNA - metabolism Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology Isomerases Isomerism Models, Molecular Molecular Structure Structure-Activity Relationship Topoisomerase I Inhibitors
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Beschreibung
Zusammenfassung:	Substituted 8-ethyl-2-(2-oxo-1,2-dihydroindol-3-ylidene)-8-hydroxy-2,3,5,8- tetrahydro-6-oxa-3a-azacyclopenta[b]naphthalene-1,4,7-triones were synthesized and evaluated as topoisomerase I inhibitors in an in vitro cleavable complex assay. The activity of these compounds may be attributed to their rigid, planar geometry, and an attempt was made to correlate the SAR in this series to known attributes of camptothecin.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00006a008