期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 2, 页码 552-557出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.11.022
关键词
Heat shock protein 90; Hsp90 inhibitors; Novobiocin analogues; Breast cancer
资金
- NIH/NCI [CA120458]
- DOD Prostate Cancer Research Program [QH815179]
Hsp90 is a promising therapeutic target for the treatment of cancer. Novobiocin is the first Hsp90 C-terminal inhibitor ever identified and recent structure-activity relationship studies on the noviose sugar identified several commercially available amines as suitable surrogates. In an effort to further understand this region of the molecule, analogues containing various N'-amino substituents were prepared and evaluated against two breast cancer cell lines for determination of their efficacy. Compound 37j manifested the most potent anti-proliferative activity from these studies and induced Hsp90-dependent client protein degradation at mid nano-molar concentrations. (C) 2012 Elsevier Ltd. All rights reserved.
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