1417646-41-3Relevant academic research and scientific papers
COUMARIN BASED HSP90 INHIBITORS WITH UREA AND ETHER SUBSTITUENTS
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, (2015/05/26)
Compounds of the formulas: wherein: R1-R4, X1, Y1, and A are as defined herein are provided. Pharmaceutical compositions of the compounds are also provided. In some aspects, these compounds are are useful for th
Novobiocin analogues with second-generation noviose surrogates
Zhao, Huiping,Blagg, Brian S.J.
, p. 552 - 557 (2013/02/23)
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.
