Synthesis and In-Vitro Biological Activity of Novel 2-Alkyl/Aryl-N-Substituted- 1Hbenzimidazole- 5-Carboxamide Derivatives as Anticancer Agents

Abstract

The primary functions of cancer chemotherapeutic agents are not only to inhibit the growth or kill the cancer cells, but conventional cancer chemotherapy is highly inadequate as a result of the lack of selectivity between cancer cells and normal cells. This calls for novel cancer therapies for selectively targeting cancers without toxicity to normal tissues. The discovery of novel anticancer agents will hopefully provide the desired degree of selectivity for cancer cells. These novel targets include genes involved in malignant transformation, cancer progression and metastasis. In addition to the identification of many novel anticancer targets, molecular biology methods have facilitated the investigation of the potential of these targets for drug discovery. Extensive literature review revealed that compounds studied for anti proliferative activity with benzimidazole moieties show potent activity. Hence 2-alkyl/aryl-Nsubstitutedbenzimidazole- 5-carboxamide derivatives were designed and synthesized. Structural elucidation of the synthesized compounds was done by spectral analysis. Anti cancer activity of compounds was evaluated in vitro on A-375 cell line [Human Malignant Melanoma; Skin], DU-145 cell line [Human; Prostate; Carcinoma], and HCT-15 cell line [Human; Colon Adenocarcinoma] by XTT assay method and Doxorubicin taking as a reference standard. Compounds with 100a, 103b, 106b, 106c, 106e showed good anti proliferative activity against all cancerous cell lines on 48 h observation bases.