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1,1′-Disubstituted azinylferrocenes: synthesis, antiaggregation and antioxidant activity

  • E. Yu. Zyryanova,
  • I. A. Utepova,
  • A. A. Musikhina,
  • N. P. Boltneva,
  • N. V. Kovaleva,
  • E. V. Rudakova,
  • O. G. Serebryakova,
  • G. F. Makhaeva,
  • M. A. Kiskin,
  • V. F. Lazarev,
  • L. S. Kuznetsova,
  • I. V. Guzhova,
  • O. N. Chupakhin

摘要

An approach to the synthesis of derivatives of unsymmetric 1,1′-disubstituted azinylferrocenes containing phenol fragments was proposed. It was found that the introduction of the quinoline or 2,2′-bipyridine moiety increases the E/Z selectivity of the reaction. The monosubstituted acetylferrocene produces the products of the pinacoline rearrangement due to the McMurry coupling, whereas only 1-azinyl-1′-{1-[(4-hydroxyphenyl)-phenylmethylene]ethyl}ferrocenes were formed in the reaction with 1-azinyl-1′-acetyl-ferrocenes. The high antioxidant activity of the synthesized compounds in the ABTS and FRAP assays and high inhibitory activity against self-aggregation of β-amyloid (1–42) was shown. Cytotoxic activity of these compounds was studied on human breast cancer cells (MCF7), non-small-cell lung cancer cells (A549), colorectal cancer cells (DLD-1), and normal dermal fibroblasts (DF-2).