Organic Letters 2006-08-03

Synthesis and biological evaluation of 10,11-methylenedioxy-14-azacamptothecin.

Mark A Elban, Wenyue Sun, Brian M Eisenhauer, Rong Gao, Sidney M Hecht

Index: Org. Lett. 8 , 3513, (2006)

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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.