Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors

Synthesis and biological evaluation of novel δ-lactam-based hydroxamic acids as inhibitors of histone deacetylase (HDAC) is reported. δ-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by co...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-08, Vol.16 (15), p.4068-4070
Hauptverfasser: Kim, Hwan Mook, Lee, Kiho, Park, Bum Woo, Ryu, Dong Kyu, Kim, Kangjeon, Lee, Chang Woo, Park, Song-Kyu, Han, Jung Whan, Lee, Hee Yoon, Lee, Hyun Yong, Han, Gyoonhee
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Sprache:eng
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Zusammenfassung:Synthesis and biological evaluation of novel δ-lactam-based hydroxamic acids as inhibitors of histone deacetylase (HDAC) is reported. δ-Lactam-based hydroxamic acids, inhibitors of histone deacetylase (HDAC), have been synthesized via ring closure metathesis of key diene intermediates followed by conversion to hydroxamic acid analogues. The hydroxamic acids 12a, 12b, and 17c showed potent inhibitory activity in HDAC enzyme assay. The hydroxamic acid 12b exhibited growth inhibitory activity on five human tumor cell lines, showing good sensitivity on the MDA-MB-231 breast tumor cell.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.04.091