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 language | English (US) |
---|---|
Pages (from-to) | 4020-4024 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 55 |
Issue number | 8 |
DOIs | |
State | Published - Apr 26 2012 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery