Synthesis of a novel fused pyrrolodiazepine-based library with anti-cancer activity

Neha Malik, Iredia D. Iyamu, Karl A. Scheidt, Gary E. Schiltz*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

5 Scopus citations


Development of drugs for new and persistent diseases will increasingly rely on the expansion of accessible chemical space to allow exploration of novel molecular targets. Here we report the synthesis of a library of novel fused heterobicyclic small molecules based on the 1,4-diazepine and 2,4-pyrrolidinedione scaffolds. Key chemical transformations included a Mannich-type condensation and chemoselective N-acylation reactions. Screening shows anti-cancer activity of several library compounds which suggests translational potential of this novel chemical scaffold.

Original languageEnglish (US)
Pages (from-to)1513-1516
Number of pages4
JournalTetrahedron Letters
Issue number15
StatePublished - Apr 11 2018


  • Cancer
  • Diazepine
  • Library
  • Mannich reaction

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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