User:Simoncaulton/sandbox
Appearance
Clinical data | |
---|---|
Trade names | Phortress |
Identifiers | |
| |
PubChem CID | |
Chemical and physical data | |
Formula | C20H24ClFN4OS |
Molar mass | 422.947 g/mol g·mol−1 |
Phortress is a 2-(4-aminophenyl)benzothiazole derivative that is currently in phase-1 clinical trials. It was developed from compound CJM 126, which was previously identified in a kinase inhibitor discovery programme. In order to improve this drug's anti-tumour activity, CJM 126 was derivatised by methylation on its phenolic ring, producing 2-(4-Amino-3-methylphenyl)benzothiazole (DF 203). DF 203 suffered from metabolism at higher concentrations, so a fluorine atom was substituted on the benzothiazole group. Finally, to improve its solubility it was conjugated to lysine forming the final drug for clinical assesment.