期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 15, 页码 4528-4532出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.05.129
关键词
Human peptide deformylase; Benzofuran-4,5-diones; Structure-activity relationships; Fluorescence polarization; Antiproliferative agents
资金
- Commonwealth Foundation for Cancer Research
- Experimental Therapeutics Center of MSKCC
- William Randolph Hearst Fund in Experimental Therapeutics
- Lilian S Wells Foundation
- NIH/NCI Cancer Center [5 P30 CA008748-44]
- NIH [1R21NS57008]
Selective inhibitors of human peptide deformylase (HsPDF) are predicted to constitute a new class of antitumor agents. We report the identification of benzofuran-4,5-diones as the first known selective HsPDF inhibitors and we describe their selectivity profile in a panel of metalloproteases. We characterize their structure-activity relationships for antitumor activity in a panel of cancer cell lines, and we assess their in vivo efficacy in a mouse xenograft model. Our results demonstrate that selective HsPDF inhibitors based on the benzofuran-4,5-dione scaffold constitute a novel class of antitumor agents that are potent in vitro and in vivo. (C) 2011 Elsevier Ltd. All rights reserved.
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