期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 8, 页码 2772-2774出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.02.086
关键词
Naphthoquinone derivatives; Antiproliferative agents; 20S Proteasome inhibitors
资金
- 863 Hi-Tech Program [SS2012AA021103]
Fourteen naphthoquinone derivatives (1-14) were designed based on a putative proteasome inhibitor PI-083. These compounds were synthesized and evaluated against A549, DU145, KB, and KBvin tumor cell lines. Six compounds (2, 4, 8, 9, 10, and 13) showed antiproliferative activities comparable to that of PI-083. Among them, compound 8 was confirmed as a 20S proteasome inhibitor in both in vitro and cell-based assays. These findings endorse further optimization efforts based on this structural phenotype to develop potential anticancer drug candidates. (C) 2012 Elsevier Ltd. All rights reserved.
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