Water-Soluble Camptothecin Derivatives that Are Intrinsic Topoisomerase I Poisons

Nicolas J. Rahier; Brian M. Eisenhauer; Rong Gao; Shannon H. Jones; Sidney M. Hecht

doi:10.1021/ol030119n

Water-Soluble Camptothecin Derivatives that Are Intrinsic Topoisomerase I Poisons

Nicolas J. Rahier, Brian M. Eisenhauer, Rong Gao, Shannon H. Jones, Sidney M. Hecht

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

22 Scopus citations

Abstract

(Matrix presented) In an effort to improve the water solubility of camptothecin, four 20-O-phosphate and phosphonate analogues have been prepared. These analogues are freely water soluble, stable at physiological pH, and stabilize the human topoisomerase I-DNA covalent binary complex with the same sequence selectivity as camptothecin itself. All four compounds inhibited the growth of yeast expressing human topoisomerase I in an enzyme-dependent fashion.

Original language	English (US)
Pages (from-to)	321-324
Number of pages	4
Journal	Organic Letters
Volume	6
Issue number	3
DOIs	https://doi.org/10.1021/ol030119n
State	Published - Feb 5 2004
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Physical and Theoretical Chemistry
Organic Chemistry

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abstract = "(Matrix presented) In an effort to improve the water solubility of camptothecin, four 20-O-phosphate and phosphonate analogues have been prepared. These analogues are freely water soluble, stable at physiological pH, and stabilize the human topoisomerase I-DNA covalent binary complex with the same sequence selectivity as camptothecin itself. All four compounds inhibited the growth of yeast expressing human topoisomerase I in an enzyme-dependent fashion.",

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AU - Rahier, Nicolas J.

AU - Eisenhauer, Brian M.

AU - Gao, Rong

AU - Jones, Shannon H.

AU - Hecht, Sidney M.

PY - 2004/2/5

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N2 - (Matrix presented) In an effort to improve the water solubility of camptothecin, four 20-O-phosphate and phosphonate analogues have been prepared. These analogues are freely water soluble, stable at physiological pH, and stabilize the human topoisomerase I-DNA covalent binary complex with the same sequence selectivity as camptothecin itself. All four compounds inhibited the growth of yeast expressing human topoisomerase I in an enzyme-dependent fashion.

AB - (Matrix presented) In an effort to improve the water solubility of camptothecin, four 20-O-phosphate and phosphonate analogues have been prepared. These analogues are freely water soluble, stable at physiological pH, and stabilize the human topoisomerase I-DNA covalent binary complex with the same sequence selectivity as camptothecin itself. All four compounds inhibited the growth of yeast expressing human topoisomerase I in an enzyme-dependent fashion.

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Water-Soluble Camptothecin Derivatives that Are Intrinsic Topoisomerase I Poisons

Abstract

ASJC Scopus subject areas

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