title: Comparative QSAR studies on bibenzimidazoles and terbenzimidazoles inhibiting topoisomerase I.
abstract: 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.
authors.affiliation: Department of Chemistry, Pomona College, Claremont, CA 91711, USA.
authors.forename: S B
authors.initials: SB
authors.lastname: Mekapati
authors.forename: C
authors.initials: C
authors.lastname: Hansch
mesh_terms: 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
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D059004:Topoisomerase I Inhibitors; D004247:DNA