Basically substituted ellipticine analogs as potential antitumor agents

Installation of a basic side chain on the ring nitrogen of ellipticine did, as expected, improve the DNA binding properties of these molecules as measured by an ethidium displacement assay. In vivo antitumor activity was not, however, improved.

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Bibliographische Detailangaben
Veröffentlicht in:	Journal of medicinal chemistry 1986-07, Vol.29 (7), p.1321-1322
Hauptverfasser:	Werbel, Leslie M, Angelo, Mario, Fry, David W, Worth, Donald F
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkaloids - chemical synthesis Animals Chemistry Drug Evaluation, Preclinical Ellipticines - chemical synthesis Ellipticines - therapeutic use Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings Indicators and Reagents Leukemia L1210 - drug therapy Magnetic Resonance Spectroscopy Mice Organic chemistry Preparations and properties Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	Installation of a basic side chain on the ring nitrogen of ellipticine did, as expected, improve the DNA binding properties of these molecules as measured by an ethidium displacement assay. In vivo antitumor activity was not, however, improved.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00157a040