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Topoisomerase I Inhibition of 2-Substituted 5-Nitrobenzimidazoles  

Edmond J. LaVoie (College of Pharmacy, Rutgers the State University of New Jersey, USA)
Publication Information
YAKHAK HOEJI / v.47, no.3, 2003 , pp. 125-129 More about this Journal
Abstract
A series of 2-phenyl-5-nitrobenzimidazoles substituted at the para positon of the 2-phenyl moiety was synthesized ＆ evaluated for their activity to inhibit topoisomerase I. The structure-activity relationship study revealed that neither the electronic nor lipophilic parameters were related to the topoisomerase I inhibition. A strict spatial requirement seems to be present for retention of topoisomerase I inhibition activity.
Keywords
2-Phenyl-5-nitrobenzimidazole; topoisomerase I inhibition; structure-activity relationship;
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