2'-Nitroflavone

2'-Nitroflavone is a PARP1 inhibitor that impedes the proliferation of triple-negative breast cancer cells, induces cell cycle arrest and apoptosis (apoptosis), and inhibits the migration of these cancer cells as well as endothelial cells. It exhibits antitumor activity and is useful for research into tumors such as triple-negative breast cancer.

2'-Nitroflavone at concentrations of 1.25-40 μM over a period of 0-96 hours reduces the viability of triple-negative breast cancer (TNBC) cells, specifically MDA-MB-231, BT-549, and MDA-MB-468, with IC50 values of 4.0 μM, 9.2 μM, and 6.5 μM after 72 hours of treatment, respectively. The compound also exhibits an IC50 of 14.5 μM on EA.hy926 endothelial cells after 96 hours. At 0-25 μM for 72-144 hours, 2'-Nitroflavone inhibits TNBC cell colony formation and migration and induces cell cycle arrest and apoptosis. Additionally, at 1-25 μM for 72 hours, it decreases α-tubulin protein levels in MDA-MB-231 and BT-549 cells, disrupts α-tubulin arrangement, and induces the formation of multipolar mitotic spindles.

In a mouse model of 4T1 triple-negative breast cancer, '2'-Nitroflavone (20 mg/kg; administered via intraperitoneal injection; 5 times a week for 2 consecutive weeks) exhibits antitumor activity.