Abstract
Chemotherapy is one of the most commonly used methods of cancer disease treatment. Due to the acquisition of drug resistance and the possibility of cancer recurrence, there is an urgent need to search for new molecules that would be more effective in destroying cancer cells. In this study, 1-(benzofuran-2-yl)ethan-1-one oxime and 26 oxime ethers containing heterocyclic, alicyclic or aromatic moiety were screened for their cytotoxicity against HeLa cancer cell line. The most promising derivatives with potential antitumor activity were 2-(cyclohexylideneaminoxy)acetic acid (18) and (E)-acetophenone O-2-morpholinoethyl oxime (22), which reduced the viability of HeLa cells below 20% of control at concentrations of 100–250 μg/mL. Some oxime ethers, namely thiazole and benzothiophene derivatives (24–27), also reduced HeLa cell viability at similar concentrations but with lower efficiency. Further cytotoxicity evaluation confirmed the specific toxicity of (E)-acetophenone O-2-morpholinoethyl oxime (22) against A-549, Caco-2, and HeLa cancer cells, with an EC50 around 7 μg/mL (30 μM). The most potent and specific compound was (E)-1-(benzothiophene-2-yl)ethanone O-4-methoxybenzyl oxime (27), which was selective for Caco-2 (with EC50 116 μg/mL) and HeLa (with EC50 28 μg/mL) cells. Considering the bioavailability parameters, the tested derivatives meet the criteria for good absorption and permeation. The presented results allow us to conclude that oxime ethers deserve more scientific attention and further research on their chemotherapeutic activity.
Highlights
The cancer diseases are a very serious health problem
Considering the bioavailability parameters, the tested derivatives met the criteria for good absorption and permeation
1-(benzofuran-2-yl)ethan-1-one oxime and 26 oxime ethers containing benzofuran, benzothiophene, thiophene, thiazole, cyclohexyl or phenyl moiety were screened for cytotoxicity against the human cervical adenocarcinoma (HeLa cell line) representative cancer cell model
Summary
The cancer diseases are a very serious health problem. About 18 million cases of various types of cancer are diagnosed each year. According to WHO predictions, this number is expected to reach 29.4 million in 2040 [1]. Chemotherapy is one of the most important methods of cancer treatment. Among the many compounds currently in use, new molecules are being developed that may be even more effective in destroying cancer cells. The problem in the treatment of neoplasms is the acquisition of drug resistance, and, the possibility of relapse of the neoplastic disease. The causes of cancer are difficult to estimate, but are certainly a very complex problem [2]. There is a need to search for and investigate new structures that offer the potential to cure cancer
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