Cancer is characterized by uncontrolled growth of abnormal cells and causes drastic changes in normal physiological function. Tumors have the propensity to spread to other organs as well, which further increases the extent of the physiological damages to essential organs. Cancer has not only become the second-leading cause of death in the United States, but it also considerably diminishes the quality of life in patients. Coupled with considerable toxicity, emergence of drug resistance continues to be a major limitation associated with cancer therapy. Despite the discovery and approval of several classes of new chemotherapeutics, there is still a considerable need for novel therapeutic options, perhaps with reduced toxicity profile and potency toward drug-resistant tumors. We have synthesized and assessed the anticancer activity of a small library of structurally unique benzimidazoles. Specifically, these compounds are designed based on a series of structural class, such as indole-2-carboxylic acid, fatty acid, and alpha-amino acids. In addition, our synthetic method involves a mild, one-pot operation that enables us to access these benzimidazoles highly efficiently. The library of compounds has been tested in three cancer cell lines: HepG2 (human hepatocellular carcinoma), HeLa (human cervical cancer) and A549 (human lung carcinoma). Many of the compounds tested showed anticancer activity in a concentration-dependent manner (IC50 < 20 µM). In addition, we have measured active caspase-3 expression and utilized a fluorescence-based apoptosis-necrosis assay to investigate the mechanism of cytotoxicity of these compounds. Most of the compounds exhibited cytotoxicity via apoptosis. Our findings suggest that further development of these test compounds could provide drug leads as new chemotherapeutic agents. 

Synthesis and biological evaluation of structurally diverse benzimidazole scaffolds as potential chemotherapeutic agents

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.