engleski

Synthesis, antioxidative and antiproliferative activity of methoxy amidino substituted benzamides and benzimidazoles

Within this manuscript the synthesis and potential antioxidative and antiproliferative activity of novel methoxy amidino substituted bezamides 6-17 and benzimidazoles 23-28 and 32-35 is presented. Their antioxidative potency has been evaluated by in vitro spectrophotometric assays and preliminary structure-activity relationships among the synthesized compounds are discussed. The compound 28 bearing three methoxy groups on a phenyl ring and imidazolinyl amidine groupe on benzimidazole nucleous directly attached to the phenyl ring exhibited the most prominent reducing activity as well as free-radical scavenging activity. Furthermore all novel compounds were tested against three human cell lines: HCT 116 (colon carcinoma), H 460 (lung carcinoma) and MCF-7 (breast carcinoma). The most prominent antiproliferative effect in the single-digit micromolar range was observed for compound 33 on MCF-7 (IC50 = 9 µM) cell line, comparable to the standard etoposide.

amidines ; benzamides ; benzimidazoles ; methoxy groups ; antioxidative activity ; antiproliferative activity

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