Three overlooked chemical approaches toward 3-naphthalimide amonafide N-derivatives

Tamara Brider, Boris Redko, Flavio Grynszpan, Gary Gellerman

Research output: Contribution to journalArticlepeer-review


Three efficient strategies for derivatization of the anticancer drug candidate amonafide (Quinamed, originally AS1413) are described. Unprecedented reductive amination of aryl aldehydes, SNAr, and addition-elimination reactions, while using readily available starting materials, give quick entry to potential libraries of novel 3-aryl, 3-benzyl N-derivatives of amonafide. The selective anticancer activity of this important DNA intercalation agent is expected to be enhanced by expanding the diversity of amonafide N-derivatives. The synthetic routes reported in this work are general and readily applicable.

Original languageEnglish
Pages (from-to)6675-6679
Number of pages5
JournalTetrahedron Letters
Issue number49
StatePublished - 3 Dec 2014


  • Addition-elimination reaction
  • Amonafide
  • Anticancer
  • DNA intercalator
  • Hybrid
  • SAr

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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