Jump to content

User:Simoncaulton/sandbox

From Wikipedia, the free encyclopedia

This is an old revision of this page, as edited by Simoncaulton (talk | contribs) at 13:50, 8 March 2018. The present address (URL) is a permanent link to this revision, which may differ significantly from the current revision.

Simoncaulton/sandbox
Clinical data
Trade namesPhortress
Identifiers
  • (2S)-2,6-diamino-N-[4-(5-fluoro-1,3-benzothiazol-2-yl)-2-methylphenyl]hexanamide;hydrochloride
PubChem CID
Chemical and physical data
FormulaC20H24ClFN4OS
Molar mass422.947 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.

CJM-126