1. Design and synthesis of stable, water soluble radicals as potential anti-cancer agents.
- Author
-
Lattmann E, Begum A, and Plater MJ
- Subjects
- Antineoplastic Agents pharmacology, Aza Compounds pharmacology, Cell Line, Drug Screening Assays, Antitumor, Free Radicals, Indicators and Reagents, Solubility, Water chemistry, Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Aza Compounds chemical synthesis, Aza Compounds chemistry, Drug Design
- Abstract
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.
- Published
- 1999