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

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

  • J Med Chem. 2012 Apr 26;55(8):4020-4. doi: 10.1021/jm300043c.
Min Jiang 1,  Bingbing X Li,  Fuchun Xie,  Frances Delaney,  Xiangshu Xiao
Affiliations

Affiliation

  • 1 Program in Chemical Biology, Oregon Health & Science University, 3181 SW Sam Jackson Park Road, Portland, Oregon, USA.
PMID: 22458559 DOI: 10.1021/jm300043c
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.

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