Synthetic thalidomide analogues (compounds 1-35), including phenylphthalimide, pyridylphthalimide, aminobenzylphthalimide, and diphenylazophthalimide, were tested for their cytotoxic effects on human cancer cell lines Hep2 (Human Larynx Carcinoma Cells), HL-60 (Human Myeloid Leukemia Cells), NUGC (Human Gastric Carcinoma Cells), and HONE-1 (Human Nasopharyngeal Carcinoma Cells) because the incidence rate is more prominent in Asian countries than in Western countries. Compounds 17, 27, 28, and 35 were found to have antitumor activity in Hep2 and HL-60 cell lines. Compounds 2, 4, 15, 17, 19, 20, 23, and 27 can inhibit nitric oxide (NO) synthase activity by more than 90%. These thalidomide analogues were found to be potent inducible nitric oxide synthase (iNOS) inhibitors, and the iNOS inhibiting potential of compounds 17 and 27 might be an advantage for anticancer therapy. In conclusion, inhibition of NO synthesis is a new development in cancer therapy for now and in the future. We modified the structures of the thalidomide analogues to have a stronger anticancer effect and a good therapeutic effect.
Previous studies indicated that cantharidin (exo-2,3-dimethy-7-oxabicyclo [2,2,1] heptane-2,3-dicarboxylic anhydride) could inhibit the proliferation of cancer cells via p53 dependent mechanism. It could also inhibit protein phosphatases 1(PP1) and protein phosphatases 2A (PP2A). When cantharidin was treated with cancer cell, it could induce to produce oxidative stress.Oxidative stress would cause damage the single and double stand DNA increasingly. But the mechanism of anticancer is still not clear. Here, cantharidin and cantharidin derivatives were served as photo-initiated DNA cleavage agents. We combined them with irradiation (λ=352nm) to see if they have the ability to cleavage the supercoiled DNA. The results displayed that the cantharidin derivatives could cleavage DNA at acidic condition with irradiation. Then, we used high-resolution gel electrophoresis to analyze the results and the experiment of Maxma-Gilbert was served as standard. The results indicated that cantharidin derivatives have better ability of cleavage at the guanine site.
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