Hypoxic Radiosensitizers: Substituted Styryl Derivatives

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

Research output: Contribution to journalArticlepeer-review

3 Scopus citations


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 languageEnglish
Pages (from-to)619-625
Number of pages7
JournalArchiv der Pharmazie
Issue number10
StatePublished - 1994


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