Identification of benzofuran-4,5-diones as novel and selective non-hydroxamic acid, non-peptidomimetic based inhibitors of human peptide deformylase Journal Article
| Authors: | Antczak, C.; Shum, D.; Bassit, B.; Frattini, M. G.; Li, Y.; de Stanchina, E.; Scheinberg, D. A.; Djaballah, H. |
| Article Title: | Identification of benzofuran-4,5-diones as novel and selective non-hydroxamic acid, non-peptidomimetic based inhibitors of human peptide deformylase |
| Abstract: | 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. © 2011 Elsevier Ltd. All rights reserved. |
| Keywords: | fluorescence polarization; structure-activity relationships; antiproliferative agents; benzofuran-4,5-diones; human peptide deformylase |
| Journal Title: | Bioorganic & Medicinal Chemistry Letters |
| Volume: | 21 |
| Issue: | 15 |
| ISSN: | 0960-894X |
| Publisher: | Pergamon-Elsevier Science Ltd |
| Date Published: | 2011-08-01 |
| Start Page: | 4528 |
| End Page: | 4532 |
| Language: | English |
| DOI: | 10.1016/j.bmcl.2011.05.129 |
| PROVIDER: | scopus |
| PMCID: | PMC3139024 |
| PUBMED: | 21719286 |
| DOI/URL: | |
| Notes: | --- - "Export Date: 17 August 2011" - "CODEN: BMCLE" - "Source: Scopus" |
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45Frattini -
499Scheinberg -
101Djaballah -
40Antczak -
351De Stanchina -
133Li -
54Shum -
7Bassit
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