Anticancer agent 71

Anticancer agent 71 (Compound 4b) is a potent anticancer agent and induces apoptosis. Anticancer agent 71 arrests cell cycle at G2/M phase and induces apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Anticancer agent 71 shows antiproliferative activity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

Anticancer agent 71 (Compound 4b) (0.1-50 μM, 24 hours; SW480 and PC3 cells) increases the cytotoxicity and exerts potent antitumor activities against SW480 and PC3 cells[1]. Anticancer agent 71 (Compound 4b) (11.08 μM, 24 hours; SW480 cells) induces a significant G2/M phase arrest[1]. Anticancer agent 71 (Compound 4b) (11.08 μM, 24 hours) induces apoptosis in SW480 cells by upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression[1]. Cell Cytotoxicity Assay[1] Cell Line: SW480 and PC3 cells Concentration: 0.1, 1, 12.5, 25 and 50 μM Incubation Time: 24 hours Result: Inhibited with IC50 values of 11.08 and 17.39 μM for SW480 and PC3 cells, respectively. Cell Cycle Analysis[1] Cell Line: SW480 cells Concentration: 11.08 μM Incubation Time: 24 hours Result: The cell population percent at G2/M phase increased to 45.3%. Apoptosis Analysis[1] Cell Line: SW480 cells Concentration: 11.08 μM Incubation Time: 24 hours Result: The percentage of cells in early and late apoptosis was recorded as 5.69% and 3.52%, respectively. Western Blot Analysis[1] Cell Line: SW480 cells Concentration: 11.08 μM Incubation Time: 24 hours Result: The expression of antiapoptotic protein Bcl-2 decreased and the expression of Pro apoptotic Bax increased.

[1]. Kilic-Kurt Z, et al. Synthesis and anticancer activity of some pyrimidine derivatives with aryl urea moieties as apoptosis-inducing agents. Bioorg Chem. 2020 Aug;101:104028.