期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 15, 页码 4068-4070出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.04.091
关键词
delta-lactam; ring closure metathesis; histone deacetylase; anticancer
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. (c) 2006 Elsevier Ltd. All rights reserved.
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