Anticanceragent 205 (compound 9) is an effective anticancer agent that binds to the G4-mtDNA target, inhibiting the replication, transcription, and translation of mtDNA (mitochondrial genome). It induces mitochondrial dysfunction, increases ROS production, and triggers DNA damage and cellular senescence. Anticanceragent 205 also promotes apoptosis and causes cell cycle arrest at the G0/G1 phase, showing potential for research in colorectal cancer.

Anticancer agent 205 (compound 9) at 4 µM interacts with G4-mtDNA in HCT116 cells within 1 hour. It also reduces mRNA levels of ND2 and ND5 in HCT116 and HFF1 cells at concentrations of 0, 1, 2, and 4 µM over 48 hours. Furthermore, it decreases protein levels of ND3, ND4, ND6, COX1, COX2, COX3, CYTB, ATP6, and ATP8 in HCT116 cells under similar conditions. The compound increases ROS levels in a concentration-dependent manner and induces DNA damage and cellular senescence at 0-4 µM over a 72-hour period.

The compound Anticancer agent 205, administered at 5 mg/kg intravenously every two days over a 16-day period, inhibits tumor growth in the HCT116 xenograft mouse model.