- 8-Aminoquinolines as anticoccidials - Part III
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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.
- 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
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- AMINOQUINOLINE DERIVED HEAT SHOCK PROTEIN 90 INHIBITORS, METHODS OF PREPARING SAME, AND METHODS FOR THEIR USE
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Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors and methods for making these classes are provided herein. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases, such as inflammation and
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Page/Page column 47-48
(2010/04/28)
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- Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling
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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.
- 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
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p. 6903 - 6910
(2008/12/22)
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