Author/Authors :
Yun-Fei Zhu، نويسنده , , Xiaochuan Wang، نويسنده , , Patrick Connors، نويسنده , , Keith Wilcoxen، نويسنده , , Yinghong Gao، نويسنده , , Raymond Gross، نويسنده , , Nathalie Strack، نويسنده , , Timothy Gross، نويسنده , , James R. McCarthy، نويسنده , , Qiu Xie، نويسنده , , Nicholas Ling، نويسنده , , Chen Chen، نويسنده ,
Abstract :
4-Benzylquinolines 5, based on a series of isoquinolines 1, were prepared and tested as inhibitors of the IGF/IGFBP-3 complex based on their ability to displace IGF-I from its binding to IGF-binding protein-3. SAR studies on the 6,7-dihydroxy moiety of the quinoline 5a showed that the catecol moiety could be replaced with other functional groups. Computational modeling of the 5a/mini-IGFBP-5 complex revealed the possible binding site of 5a on IGFBP-5.