Anticancer agent 47

Anticancer agent 47 (compound 4j) is a potent anticancer agent. Anticancer agent 47 shows antiproliferative activities. Anticancer agent 47 induces apoptosis and cell cycle arrest at G0/G1 phase. Anticancer agent 47 shows shows antitumor activities in vivo[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Anticancer agent 47 (compound 4j) shows antiproliferative activities with IC50s of 1.6, 0.72, 7.07 µM for HepG2, A549, H596 cells, respectively[1]. Anticancer agent 47 (0.8, 1.6, 3.2 µM; 24 h) induces apoptosis and cell cycle arrest at G0/G1 phase[1]. Anticancer agent 47 (5 µM; 5h) significantly increases ROS production[1]. Apoptosis Analysis[1] Cell Line: HepG2, H596 cells Concentration: 0.8, 1.6, 3.2 µM Incubation Time: 24 h Result: Induced apoptosis with the apoptotic cell rates were 14.23, 20.47 and 27.66% at 0.8, 1.6, 3.2 µM in HepG2 cell, respectively. Cell Cycle Analysis[1] Cell Line: HepG2 cells Concentration: 0.8, 1.6, 3.2 µM Incubation Time: 24 h Result: Showed 48.54%, 49.60% and 53.00% cells were at G0/G1 phase at 0.6, 1.2 and 2.4 µM, respectively.

Anticancer agent 47 (20 mg/kg; i.v.; once every 2 days for 19 days) shows antitumor activities[1]. Animal Model: BALB/c nude mice (HepG2 xenografts)[1] Dosage: 20 mg/kg Administration: I.v.; once every 2 days for 19 days Result: Effectively inhibited tumor growth with the 58.7% tumor inhibition rate.

[1]. Wu L, et al. Synthesis and biological evaluation of β-lapachone-monastrol hybrids as potential anticancer agents. Eur J Med Chem. 2020 Oct 1;203:112594.