35868-49-6Relevant articles and documents
Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling
Ganesh, Thota,Min, Jaeki,Thepchatri, Pahk,Du, Yuhong,Li, Lian,Lewis, Iestyn,Wilson, Larry,Fu, Haian,Chiosis, Gabriela,Dingledine, Raymond,Liotta, Dennis,Snyder, James P.,Sun, Aiming
, p. 6903 - 6910 (2008)
The molecular chaperone Hsp90 plays important roles in maintaining malignant phenotypes. Recent studies suggest that Hsp90 exerts high-affinity interactions with multiple oncoproteins, which are essential for the growth of tumor cells. As a result, research has focused on finding Hsp90 probes as potential and selective anticancer agents. In a high-throughput screening exercise, we identified quinoline 7 as a moderate inhibitor of Hsp90. Further hit identification, SAR studies, and biological investigation revealed several synthetic analogs in this series with micromolar activities in both fluorescent polarization (FP) assay and a cell-based Western blot (WB) assay. These compounds represent a new class of Hsp90 inhibitors with simple chemical structures.
