Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors |
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Authors: | 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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Institution: | Korea Research Institute of Bioscience and Biotechnology, Yuseong, Daejeon 305-333, Republic of Korea. |
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Abstract: | delta-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. |
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