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Synthesis and biological evaluation of 10,11-methylenedioxy-14-azacamptothecin
Mark A Elban1, Wenyue Sun, Brian M Eisenhauer
1Department of Chemistry, University of Virginia, Charlottesville, Virginia 22904, USA.
Organic Letters
|July 28, 2006
Abstract:
[reaction: see text] 10,11-Methylenedioxy-14-azacamptothecin, a potent analogue of the antitumor agent camptothecin (CPT), has been prepared via a key condensation between AB and DE ring precursors. The biological testing of this compound validated a strategy for modulation of the off-rate of camptothecin analogues from the topoisomerase-DNA-CPT ternary complex via structural modification.
