Antiproliferative agent-76

Antiproliferative agent-76 (Compound II-2) is an 8-sulfonamidoquinolin derivative and a selective anticancer agent. It can inhibit the NF-κB and WNT signaling pathways, promoting apoptosis in cancer cells. Antiproliferative agent-76 exhibits anticancer activity against colorectal cancer and leukemia.

Antiproliferative agent-76 at a concentration of 10 μM over 48 hours effectively inhibits the proliferation of HCT116 colorectal cancer cells with an IC50 of 1.0 ± 0.13 μM, and for HT-29 colorectal cancer cells, the IC50 is 5.3 ± 0.84 μM. It also suppresses the growth of Mv4;11 myeloid leukemia cells, exhibiting an IC50 of 7.6 ± 0.65 μM. When applied at 10 μM, this agent selectively inhibits the proliferation of eight cancer cell lines, achieving inhibition rates exceeding 80%, while showing low activity on normal 786-O and L-02 cells. Additionally, Antiproliferative agent-76 at concentrations of 1.25-5 μM over 48 hours induces apoptosis in HCT116 colorectal cancer cells, with an apoptosis rate reaching 80% after 48 hours at 5 μM. Moreover, Antiproliferative agent-76 (II-2) at concentrations of 1.25-2.5 μM over 48 hours causes a concentration-dependent G2/M phase cell cycle arrest in HCT116 colorectal cancer cells.