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

Research output: Contribution to journalArticle

16 Citations (Scopus)

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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Cyclic AMP Response Element-Binding Protein
Genes
Neoplasms
Pharmaceutical Preparations
naphthol AS-E

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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Design, synthesis, and biological evaluation of conformationally constrained analogues of naphthol AS-E as inhibitors of CREB-mediated gene transcription. / Jiang, Min; Li, Bingbing X.; Xie, Fuchun; Delaney, Frances; Xiao, Xiangshu.

In: Journal of Medicinal Chemistry, Vol. 55, No. 8, 26.04.2012, p. 4020-4024.

Research output: Contribution to journalArticle

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