Design and synthesis of stable, water soluble radicals as potential anti-cancer agents.
A free diazafluorenyl radical based on the Koelsch free radical was designed and synthesized with expectations of stability and water solubility. The novel radical precursors were synthesised from the parent brominated stilbene and the substituted fluorenes in an IPSO substitution, as a key synthetic step. The precursors were deprotonated and the anion was discharged by an aqueous solution of potassium cyanoferrate. The new radicals were prepared from fluorene in 6 steps with good overall yields. These radicals have shown promising anticancer activity in initial screenings on 2 different MAC cell lines.
Lattmann
E
E
Pharmaceutical Sciences Research Institute, Aston University, Birmingham, England. e.lattmann@aston.ac.uk
Begum
A
A
Plater
M J
MJ
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D005609:Free Radicals; D007202:Indicators and Reagents; D012995:Solubility; D014867:Water / Q000737:chemistry
D000970:Antineoplastic Agents; D001372:Aza Compounds; D005609:Free Radicals; D007202:Indicators and Reagents; D014867:Water