Anticancer agent 69 (Compound 34) is an effective selective anticancer agent with selective inhibition on human prostate cancer cell line PC3 (IC50=26 nM). Anticancer agent 69 can increase ROS level and down-regulate EGFR, thus inducing apoptosis.

Anticancer agent 69 (Compound 34, 0-20 μM approximately, 72 h) has selective anticancer activity in PC3 cells with an IC 50 value of 26 nM against other cancer cell lines and normal cell lines [1]. Anticancer agent 69 (1-7 days) inhibits the cell viabilities of PC3 cells and PC9 cells in a time- and dose-dependent manne [1]. Anticancer agent 69 (0-100 nM, 7 days) forms fewer and smaller colonies compared those with DMSO-treated cells [1]. Anticancer agent 69 (0-800 nM, 34/72 h) increases ROS production, and further stimulates Prx I-III expression, phosphorylation level of MAPK ‘s downstream proteins, expression of apoptosis-related proteins [1]. Anticancer agent 69 (0-500 nM, 72 h) decreases the level of EGFR and phosphorylation level of its downstream protein (ERK, AKT), and induces PC3 cells and PC9 cells apoptosis in a dose-dependent manner [1]. Western Blot Analysis [1] Cell Line: PC3, PC9 Concentration: 0-800 nM Incubation Time: 72 h Result: Stimulated Prx I-III expression, phosphorylation level of MAPK ‘s downstream proteins (P38, JNK), expression of apoptosis-related proteins (Bax, cleaved-Caspased 3). Inhibited the level of EGFR and its downstream protein (p-ERK, p-AKT). Increased pro-apoptotic proteins (Bax and P53) expression and reduces anti-apoptotic protein (Bcl-2) expression. Cell Proliferation Assay [1] Cell Line: PC3, PC9 Concentration: 0-100 nM Incubation Time: 7 days Result: Formed fewer and smaller colonies compared those with DMSO-treated cells. Cell Viability Assay [1] Cell Line: Cancer cell lines (PC3, MGC-803, PC9, EC9706, SMMC-7721), normal cell lines (Het-1A, L02 and GES-1) Concentration: 0-20 μM approximately Incubation Time: 72 h Result: Inhibited proliferation of multiple cancer cell lines with IC 50 values of 26 nM (PC3), 557 nM (MGC-803), 148 nΜ (PC9), 3.99 μΜ (EC9706), 844 nΜ (SMMC-7721), respectively. Displayed good selectivity against normal cell lines with IC 50 values of > 20 μΜ (L02), > 5 μΜ (Het-1A), 1.57 μΜ (GES-1), respectively.