Cytotoxicity Of32Novel Synthesized Thiochromanone Derivatives On12Human Tumor Cell Lines And Underlying Mechanism

We have investigated the anti-proliferative activities of32Novel synthesizedThiochromanone Derivatives in vitro. MTT assay was used to test the inhibitory effect of32compounds on13tumor cell lines.6tested chemicals (18-22&45) showed cell toxicity to11human tumor cell lines (A549, SGC-7901, BGC-823, K562,U937, Hela, MCF-7, HepG-2,A375, LS174T, HT1080&786O), and the half maximal inhibitory concentration (IC50)values were between1.3-49.0μM.4tested chemicals (23,24,29,30) showed excellentactivities against the7human tumor cell lines in vitro, the half maximal inhibitoryconcentration (IC50) were between1.39-21.04μM;6tested chemicals (50-54&59) showedcell toxicity to10human tumor cell lines, and the half maximal inhibitory concentration(IC50) values were between1.3-37.0μM.2tested chemicals(CMDMT&CMDCT) showedthe inhibitory effect on6human tumor cell lines, and the half maximal inhibitoryconcentration (IC50) values were between8.34-24.29μM. The inhibition effects of thechemicals on tumor cells were much higher than cisplatin at the same concentration. Theother14chemicals have no effects on the growth of human tumor cell lines in vitro.We studied the effect of CMDMT on inducing apoptosis in human liver cancer cell lineHepG-2at the same time. The trypan blue exclusion method was used to count the number ofviable and dead cells for drawing cell growth curve. The cell apoptosis on morphology wasdetected by TUNEL assay. The percentage of apoptosis of human liver cancer cell lineHepG-2was measured by FCM. The amount of caspase-3in HepG-2cells was measured withELISA. The results showed that CMDMT could induce the HepG-2cell apoptosis, whichsuggested the chemical to be potential anticancer lead compound.