noviose and Breast-Neoplasms

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.

Topics: Breast Neoplasms; Cell Line, Tumor; Cell Proliferation; Female; Humans; Molecular Structure; Monosaccharides; Novobiocin; Structure-Activity Relationship