618886-07-0Relevant academic research and scientific papers
Discovery of quinolinediones exhibiting a heat shock response and angiogenesis inhibition
Hargreaves, Robert H. J.,David, Cynthia L.,Whitesell, Luke J.,LaBarbera, Daniel V.,Jamil, Akmal,Chapuis, Jean C.,Skibo, Edward B.
, p. 2492 - 2501 (2008/12/21)
A series of substituted quinoline-5,8-diones were synthesized and evaluated as inhibitors of the chaperone protein Hsp90 using two assays: competition for binding to C-terminal ATP-binding site and competition for binding to N-terminal ATP-binding site. I
Design of quinolinedione-based geldanamycin analogues
Hargreaves, Robert,David, Cynthia L.,Whitesell, Luke,Skibo, Edward B.
, p. 3075 - 3078 (2007/10/03)
Quinoline-5,8-dione-based compounds were designed from the structure of the geldanamycin-bound Hsp-90 active site. The active site model predicted that aromatic substituents should be present at the 2-position, to take advantage of a hydrophobic pocket, a
