Premium
Hypoxic Radiosensitizers: Substituted Styryl Derivatives
Author(s) -
Nudelman Abraham,
Falb Eliezer,
Odesa Yael,
ShmueliBroide Naomi
Publication year - 1994
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19943271004
Subject(s) - misonidazole , chemistry , stereochemistry , ethanolamines , derivative (finance) , medicinal chemistry , combinatorial chemistry , organic chemistry , biochemistry , in vitro , ethanolamine , economics , financial economics
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.