Synthesis of diverse lactam carboxamides leading to the discovery of a new transcription-factor inhibitor

Pui Yee Ng, Yuchen Tang, Wendy M. Knosp, H. Scott Stadler, Jared T. Shaw

Research output: Contribution to journalArticle

63 Scopus citations

Abstract

(Chemical Equation Presented) Diversity is the key: Skeletal diversity is a useful starting point in the search for compounds that modulate protein-biopolymer interactions. A library of 400 lactam carboxamides has been synthesized in a short synthetic sequence and a new compound that inhibits the interaction of a transcription factor (HOXA13) with its DNA target has been discovered, and inhibition of transcription is demonstrated in cells.

Original languageEnglish (US)
Pages (from-to)5352-5355
Number of pages4
JournalAngewandte Chemie - International Edition
Volume46
Issue number28
DOIs
StatePublished - 2007

Keywords

  • Combinatorial chemistry
  • DNA
  • Gene expression
  • Lactams
  • Proteins

ASJC Scopus subject areas

  • Chemistry(all)

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