Comparative QSAR studies on bibenzimidazoles and terbenzimidazoles inhibiting topoisomerase I.
Terbenzimidazoles that inhibit topoisomerase are of interest as anticancer drugs. We have reviewed the literature and have developed 13 quantitative structure-activity relationships (QSARs) on cleaving DNA or inhibiting the growth of tumor cell cultures. The results are correlated with octanol/water partition coefficients or molecular refractivity. Suggestions have been made for the development of improved derivatives.
Mekapati
S B
SB
Department of Chemistry, Pomona College, Claremont, CA 91711, USA.
Hansch
C
C
D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology*; D002417:Cattle; D004247:DNA / Q000187:drug effects / Q000378:metabolism; D004926:Escherichia coli / Q000201:enzymology; D006801:Humans; D020128:Inhibitory Concentration 50; D021281:Quantitative Structure-Activity Relationship; D059004:Topoisomerase I Inhibitors; D014407:Tumor Cells, Cultured / Q000187:drug effects
D000970:Antineoplastic Agents; D001562:Benzimidazoles; D059004:Topoisomerase I Inhibitors; D004247:DNA