86-78-2Relevant 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 (2008/12/22)
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.
8-Aminoquinolines as anticoccidials - Part III
Armer, Richard E.,Barlow, Jacqueline S.,Chopra, Narinder,Dutton, Christopher J.,Greenway, David H.J.,Greenwood, Sean D.W.,Lad, Nita,Shaw, Jonothan,Thompson, Adrian P.,Thong, Kam-Wah,Tommasini, Ivan
, p. 2425 - 2430 (2007/10/03)
Analogues of the antimalarial pentaquine, 1, in which the nature of the side-chain on the 8-amino position was varied, were prepared and evaluated for anticoccidial activity both in vitro and in vivo. Specifically, both the inter-nitrogen distance and the nature of the terminal amino group were investigated. Novel analogues of equal or improved efficacy in vitro and in vivo to pentaquine were discovered.
