Abstract
CREB is a transcription factor implicated in the pathogenesis of multiple cancers. Targeting CREB is a promising strategy to develop potential cancer therapeutics. Previously, we identified 666-15 as a potent CREB inhibitor. Herein, we designed an ester prodrug of 666-15 through a long-range O,N-acyl transfer reaction for improved aqueous solubility. Unexpectedly, we discovered a small molecule 11 (653-47) that can potentiate the CREB inhibitory activity of 666-15 although 653-47 alone does not inhibit CREB.
Original language | English (US) |
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Pages (from-to) | 11423-11429 |
Number of pages | 7 |
Journal | Journal of Medicinal Chemistry |
Volume | 62 |
Issue number | 24 |
DOIs | |
State | Published - Dec 26 2019 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery