Preliminary Study On The Anti-tumor Function Of Hydroxyurea Derivatives

Objective:To detect the anti-tumor activity of hydroxyurea derivatives in vito and screenout the hydroxyurea derivatives that can inhibit the tumor cell through MTT assay.Research the cell apoptosis effects of hydroxyurea derivatives that have beenscreened out.Methods:（1）Hydroxyurea derivatives were screened in vitro antitumor activities againstHep-2cells, L1210cells and K562cells through MTT assay, and screened out theeffected hydroxyurea derivatives, the IC₅₀value on Hep-2cells, L1210cells andK562cells were calculated.（2）The anti-tumor action mechanism of hydroxyurea derivatives on K562cellswere investigated. Annexin V–FITC/PI staining was performed to confirm theapoptosis of K562cells incubates with YB5é—´.Results:（1）We found that thirteen kinds of hydroxyurea derivatives showed inhibitionagainst Hep-2cells, nine kinds of hydroxyurea derivatives showed inhibition againstK562cells and one kind of hydroxyurea derivative showed inhibition against L1210cells. The IC50value on Hep-2cells, L1210cells and K562cells were calculated,these compounds possess certain antitumor activity in vitro.（2）The results of AnnexinV-FITC/PI double staining FCM assay showed thatYB5é—´can induce apoptosis of K562cells compared with HU when it was treated for24hours.Its effect of inducing K562cells was outstanding,especially at theconcentration of10^-2M, and the apoptosis rates of YB5é—´was higher than that of HU.And apoptosis rates significantly increased with increasing concentration of YB₅间．Conclusion:（1）YV5、YL₅、YL₅邻、YG₁、YL3、HY-CN、HX-CN、HX-叔、YV₁、YB₄、YV₃环、YL₂and YL₅对have a very good inhibitory effect on Hep-2cells.HY-CN、 HY-CL、YG₅邻、YB₁、YB₂、YG2、YV2、YB4and YB₅é—´have a very good inhibitoryeffect on K562cells.YB₅é—´have a very good inhibitory effect on L1210cells.（2）The effect of inducing K562cells of YB₅é—´was superior to than that of HU.