Abstract
A novel series of HDAC inhibitors demonstrating class I and IIb subtype selectivity have been identified using a scaffold-hopping strategy. Several designed compounds showed better selectivity for class I and IIb over class IIa HDAC isoforms comparing to the FDA approved HDAC targeting drug SAHA. A representative lead compound 22 bearing a biphenyl moiety demonstrated promising class I and IIb HDAC isoforms selectivity and in vitro anticancer activities against several cancer cell lines. This work could serve as a fundamental platform for further exploration of selective HDAC inhibitors using designed molecular scaffold.
Original language | English (US) |
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Pages (from-to) | 639-652 |
Number of pages | 14 |
Journal | European Journal of Medicinal Chemistry |
Volume | 86 |
DOIs | |
State | Published - Oct 30 2014 |
Keywords
- HDAC
- Isoforms selectivity
- Scaffold-hopping
- Structureeactivity relationship
ASJC Scopus subject areas
- Pharmacology
- Drug Discovery
- Organic Chemistry