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

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

doi:10.1021/ol0611604

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

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

Research output: Contribution to journal › Article › peer-review

38 Scopus citations

Abstract

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.

Original language	English (US)
Pages (from-to)	3513-3516
Number of pages	4
Journal	Organic Letters
Volume	8
Issue number	16
DOIs	https://doi.org/10.1021/ol0611604
State	Published - Aug 3 2006
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Physical and Theoretical Chemistry
Organic Chemistry

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10.1021/ol0611604

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abstract = "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.",

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AU - Elban, Mark A.

AU - Sun, Wenyue

AU - Eisenhauer, Brian M.

AU - Gao, Rong

AU - Hecht, Sidney M.

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AB - 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.

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

Abstract

ASJC Scopus subject areas

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