• Media type: E-Article
  • Title: Synthesis of (3′,3′‐Dimethyloxiranyl)quinones and (Dimethylacetyl)quinones as Potential Cytostatics
  • Contributor: Kloc, Krystian; Młochowski, Jacek; Syper, Ludwik; Mordarski, Marian
  • Published: Wiley, 1986
  • Published in: Journal für Praktische Chemie, 328 (1986) 3, Seite 419-429
  • Language: English
  • DOI: 10.1002/prac.19863280318
  • ISSN: 0021-8383
  • Origination:
  • Footnote:
  • Description: Abstract1,4‐Benzoquinones and 1,4‐naphthoquinones carrying 3′,3′‐dimethyloxiranyl, dimethylacetyl or oxiranylmethyloxy substituents (1, 2 or 3) have been synthesized. The methods presented involved epoxidation of a sterically overcrowded double bond as a crucial step for synthesis of (3′,3′‐dimethyloxiranyl)quinones 1. Reaction of aryllithium derivatives with 2‐chloro‐2‐methyl‐propanol unexpectedly led to (dimethyl)acetylarenes 11 subsequently oxidized to (dimethylacetyl)‐quinones 2. High cytotoxicity of 1 against KB cells has been revealed contrary to significantly lower activity of 2 and 3. The structure‐activity relationship was discussed in terms of current theory of biologically activated alkylating agents.