In Vitro: Antiproliferative agent-23 (72 hours) has vitro antiproliferative effect in HepG2 (IC50=0.86), MDA-MB-231 (IC50=1.53), MCF-7 (IC50=0.94), A2780 (IC50=0.88), A549 (IC50=0.23), A549/CDDP (IC50=0.35), HepG2/CDDP (IC50=1.16), HUEVC (IC50=5.68). Antiproliferative agent-23 (5 μM; 24 hours) effectively induces cell apoptosis in A549/CDDP cells. Antiproliferative agent-23 (5 μM; 24 hours) can efficiently cause DNA damage in A549/CDDP cells and thus ultimately triggered apoptosis. Antiproliferative agent-23 causes a significant increase in the ER stress-related protein expression. Antiproliferative agent-23 (10, 20 μM; 24 hours) leads to inhibitory effects of polymerization with an IC50 of 9.86 μM. Antiproliferative agent-23 (5 μM; 24 hours) significantly increases intracellular ROS in A549/CDDP cells. Antiproliferative agent-23 (1 μM; 24 hours) potently inhibits A549 cell migration in in vitro assays.
In Vivo: Antiproliferative agent-23 (12.40 mg/kg; IV; every 7 days for 28 consecutive days) has antitumor efficacy and retaines the high antitumor efficiency to attenuate CDDP resistance.