Design of quinolinedione-based geldanamycin analogues.
Design of quinolinedione-based geldanamycin analogues.
复制标题
基于喹啉二酮的格尔德霉素类似物的设计。
DOI：
10.1016/s0960-894x(03)00650-4
复制
发表时间：
2003
影响因子：
2.7
通讯作者：
Skibo,EdwardB
中科院分区：
文献类型：
--
作者：
Hargreaves,Robert;David,CynthiaL;Whitesell,Luke;Skibo,EdwardB
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, and amino substituents should be present at the 6- or 7-position. COMPARE analysis revealed that the LC50profile of 2-phenyl-6-(2-chloroethylamino)quinoline-5,8-dione has the highest geldanamycin-like activity (0.74 correlation coefficient).
