Hypoxic Radiosensitizers: Substituted Styryl Derivatives

Abraham Nudelman; Eliezer Falb; Yael Odesa; Naomi Shmueli‐Broide

doi:10.1002/ardp.19943271004

Hypoxic Radiosensitizers: Substituted Styryl Derivatives

Abraham Nudelman
, Eliezer Falb
, Yael Odesa
, Naomi Shmueli‐Broide

Department of Chemistry

Bar-Ilan University

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

3 Scopus citations

Abstract

A number of novel styryl epoxides, N‐substituted‐styryl‐ethanolamines, N‐mono and N,N′‐bis‐(2‐hydroxyethyl)‐cinnamamides ‐ analogues to the known radiosensitizers RSU‐ 1069, pimonidazole and etanidazole ‐ display selective hypoxic radiosensitizing activity. The styryl group, especially when substituted by electron withdrawing groups, was found to be bioisosteric to the nitroimidazolyl functionality. The most active derivative 2‐(2′‐nitrophenyl)ethen‐1‐yl‐oxirane 8a displayed a sensitizer enhancement ratio (SER) of 5 relative to misonidazole.

Original language	English
Pages (from-to)	619-625
Number of pages	7
Journal	Archiv der Pharmazie
Volume	327
Issue number	10
DOIs	https://doi.org/10.1002/ardp.19943271004
State	Published - Oct 1994

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title = "Hypoxic Radiosensitizers: Substituted Styryl Derivatives",

abstract = "A number of novel styryl epoxides, N‐substituted‐styryl‐ethanolamines, N‐mono and N,N′‐bis‐(2‐hydroxyethyl)‐cinnamamides ‐ analogues to the known radiosensitizers RSU‐ 1069, pimonidazole and etanidazole ‐ display selective hypoxic radiosensitizing activity. The styryl group, especially when substituted by electron withdrawing groups, was found to be bioisosteric to the nitroimidazolyl functionality. The most active derivative 2‐(2′‐nitrophenyl)ethen‐1‐yl‐oxirane 8a displayed a sensitizer enhancement ratio (SER) of 5 relative to misonidazole.",

author = "Abraham Nudelman and Eliezer Falb and Yael Odesa and Naomi Shmueli‐Broide",

year = "1994",

month = oct,

doi = "10.1002/ardp.19943271004",

language = "אנגלית",

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AU - Falb, Eliezer

AU - Odesa, Yael

AU - Shmueli‐Broide, Naomi

PY - 1994/10

Y1 - 1994/10

N2 - A number of novel styryl epoxides, N‐substituted‐styryl‐ethanolamines, N‐mono and N,N′‐bis‐(2‐hydroxyethyl)‐cinnamamides ‐ analogues to the known radiosensitizers RSU‐ 1069, pimonidazole and etanidazole ‐ display selective hypoxic radiosensitizing activity. The styryl group, especially when substituted by electron withdrawing groups, was found to be bioisosteric to the nitroimidazolyl functionality. The most active derivative 2‐(2′‐nitrophenyl)ethen‐1‐yl‐oxirane 8a displayed a sensitizer enhancement ratio (SER) of 5 relative to misonidazole.

AB - A number of novel styryl epoxides, N‐substituted‐styryl‐ethanolamines, N‐mono and N,N′‐bis‐(2‐hydroxyethyl)‐cinnamamides ‐ analogues to the known radiosensitizers RSU‐ 1069, pimonidazole and etanidazole ‐ display selective hypoxic radiosensitizing activity. The styryl group, especially when substituted by electron withdrawing groups, was found to be bioisosteric to the nitroimidazolyl functionality. The most active derivative 2‐(2′‐nitrophenyl)ethen‐1‐yl‐oxirane 8a displayed a sensitizer enhancement ratio (SER) of 5 relative to misonidazole.

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JO - Archiv der Pharmazie

JF - Archiv der Pharmazie

IS - 10

ER -

Hypoxic Radiosensitizers: Substituted Styryl Derivatives

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