engleski

Antitumor activity of novel benzimidazole amidine derivatives of 7‐chloro‐4‐ aminoquinoline

As a part of our ongoing effort to prepare novel biologically active compounds, we have synthesized a short series of hybrid molecules in which 7‐chloro‐4‐aminoquinoline is linked to benzimidazole amidine moiety via m‐phenyl linker [1]. Several 7‐chloro‐4‐aminoquinoline based antimalarial therapeutics are tested for their anticancer activity, two of them (chloroquine and hydroxychloroquine) are currently investigated in clinical trials for cancer therapy [2]. Benzimidazole moiety is found in many known pharmaceuticals displaying, besides anticancer, a variety of biological effects [3]. Positively charged amidine groups are known for their cellular and nuclear uptake. Novel compounds were evaluated for their in vitro cytotoxic activity against normal epithelial (MDCK1) and carcinoma (HeLa, CaCo2, SW‐620, MCF‐7 and MDAMB231) cell lines using MTT assay.

hybrid molecules, 7‐chloro‐4‐aminoquinoline, benzimidazole amidines, anticancer activity

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