title: Benzimidazole condensed ring systems. XII. Synthesis and anticancer evaluation of certain pyrido[1,2-a]benzimidazole derivatives.
abstract: Previously, we have evaluated several pyrido[1,2-a]benzimidazoles (PBIs) as potential antineoplastic agents. Among them, NSC 649900 and NSC 682011 revealed good antineoplastic activity against some cell lines of clinically isolated human tumors. For further structure-activity relationship (SAR) studies we report here the synthesis and antineoplastic evaluation of related series of PBIs with similar haloarylamino (13-18, 23-28), haloarylaminomethylene (29-34) and haloarylazo (35-38) moieties at position 1 or 2. Some of these derivatives revealed notable activity against some tumor cell lines; the highest activity was recorded for the p-fluorophenylamino-3-phenyl-PBI (23, NSC 699944) and its p-chlorophenyl analog (24, NSC 699948). These compounds were selected by the NCI for further testing in a new in vivo anticancer hollow fiber assay.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Egypt.
authors.forename: S A
authors.initials: SA
authors.lastname: el-Hawash
authors.forename: A
authors.initials: A
authors.lastname: Badawey el-S
authors.forename: T
authors.initials: T
authors.lastname: Kappe
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles