Title of article :
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel δ-lactam-based histone deacetylase (HDAC) inhibitors
Author/Authors :
Hwan-Mook Kim، نويسنده , , Kiho Lee، نويسنده , , Bum Woo Park، نويسنده , , Dong Kyu Ryu، نويسنده , , Kangjeon Kim، نويسنده , , Chang Woo Lee، نويسنده , , Song Kyu Park، نويسنده , , Jung Whan Han، نويسنده , , Hee-Yoon Lee، نويسنده , , Hyun Yong Lee، نويسنده , , Gyoonhee Han، نويسنده ,
Abstract :
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.
Keywords :
?-Lactam , Histone deacetylase , anticancer , Ring closure metathesis
