Design, synthesis, and biological evaluation of conformationally constrained analogues of naphthol AS-E as inhibitors of CREB-mediated gene transcription

Min Jiang, Bingbing X. Li, Fuchun Xie, Frances Delaney, Xiangshu Xiao

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Abstract

Cyclic AMP response element binding protein (CREB) is often dysregulated in cancer cells and is an attractive cancer drug target. Previously, we described naphthol AS-E (1) as a small molecule inhibitor of CREB-mediated gene transcription. To understand its bioactive conformation, a series of conformationally constrained analogues of 1 were designed and synthesized. Biological evaluation of these analogues suggests that the global energy minimum of 1 is the likely bioactive conformation.

Original languageEnglish (US)
Pages (from-to)4020-4024
Number of pages5
JournalJournal of Medicinal Chemistry
Volume55
Issue number8
DOIs
StatePublished - Apr 26 2012

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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