TY - JOUR
T1 - Hypoxic Radiosensitizers
T2 - Substituted Styryl Derivatives
AU - Nudelman, Abraham
AU - Falb, Eliezer
AU - Odesa, Yael
AU - Shmueli‐Broide, Naomi
PY - 1994
Y1 - 1994
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.
UR - http://www.scopus.com/inward/record.url?scp=0028149587&partnerID=8YFLogxK
U2 - 10.1002/ardp.19943271004
DO - 10.1002/ardp.19943271004
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C2 - 7826196
AN - SCOPUS:0028149587
SN - 0365-6233
VL - 327
SP - 619
EP - 625
JO - Archiv der Pharmazie
JF - Archiv der Pharmazie
IS - 10
ER -