Phortress (2-(4-aminophenyl)benzothiazoles)

Phortress is the lead compound from work by our group on 2-(4-aminophenyl)benzothiazole compounds as anti-cancer agents. It is a water soluble pro-drug of the active moiety, a compound designated 5F 203.

Phortress has a distinctive mechanism of action whereby in tumour cells sensitive to the drug the active moiety binds to aryl hydrocarbon receptors in the cytoplasm and is subsequently translocated into the cell nucleus, where it induces its own activation via cytochrome P450 1A1. The resulting electrophilic intermediate species form DNA adducts leading to highly selective cell death.

Phortress is synthetically accessible and has been formulated for intravenous administration.

Preclinical studies (in vitro and in vivo) by both Cancer Research UK and NCI in the US have shown Phortress to be a potent anti-cancer agent, particularly against ovarian and breast cancer.