1. Synthesis and Evaluation of the Antitumor Activity of Novel 1-(4-Substituted phenyl)-2-ethyl Imidazole Apoptosis Inducers In Vitro.
- Author
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Li ZW, Zhong CY, Wang XR, Li SN, Pan CY, Wang X, and Sun XY
- Subjects
- Antineoplastic Agents chemistry, Antineoplastic Agents pharmacology, Cell Line, Tumor, Cell Proliferation drug effects, Drug Screening Assays, Antitumor, Fluorouracil pharmacology, Humans, Imidazoles chemical synthesis, Imidazoles pharmacology, Structure-Activity Relationship, Antineoplastic Agents chemical synthesis, Apoptosis drug effects, Imidazoles chemistry
- Abstract
Novel imidazole derivatives were designed, prepared, and evaluated in vitro for antitumor activity. The majority of the tested derivatives showed improved antiproliferative activity compared to the positive control drugs 5-FU and MTX. Among them, compound 4f exhibited outstanding antiproliferative activity against three cancer cell lines and was considerably more potent than both 5-FU and MTX. In particular, the selectivity index indicated that the tolerance of normal L-02 cells to 4f was 23-46-fold higher than that of tumor cells. This selectivity was significantly higher than that exhibited by the positive control drugs. Furthermore, compound 4f induced cell apoptosis by increasing the protein expression levels of Bax and decreasing those of Bcl-2 in a time-dependent manner. Therefore, 4f could be a potential candidate for the development of a novel antitumor agent.
- Published
- 2020
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