Rigid Analogs of Camptothecin as DNA Topoisomerase I Inhibitors

Citations Over TimeTop 18% of 1995 papers

Abstract

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.

Related Papers

• Protein-linked DNA strand breaks induced in mammalian cells by camptothecin, an inhibitor of topoisomerase I.(1989)
• → Inhibition of Topoisomerase I Function by Coralyne and 5,6-Dihydrocoralyne(1996)55 cited
• → Development of a stable camptothecin-resistant subline of P388 leukemia with reduced topoisomerase I content.(1990)127 cited
• → On the role of E-ring oxygen atoms in the binding of camptothecin to the topoisomerase I–DNA covalent binary complex(2004)14 cited
• → Synthesis of novel water-soluble 7-(aminoacylhydrazono)-formyl camptothecins with potent inhibition of DNA topoisomerase I(1994)24 cited