Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): synthesis, biology, and molecular modeling

…, P Thepchatri, Y Du, L Li, I Lewis, L Wilson, H Fu…

Index: 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 Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6903 - 6910

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Citation Number: 23

Abstract

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. ...