DESIGN, SYNTHESIS, AND BINDING-AFFINITY OF A NONPEPTIDE MIMIC OF SOMATOSTATIN

被引:54
作者
PAPAGEORGIOU, C
HALTINER, R
BRUNS, C
PETCHER, TJ
机构
[1] Sandoz Pharma Ltd. Preclinical Research
关键词
D O I
10.1016/S0960-894X(01)80435-2
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The tetrasubstituted xylofuranose 4 was synthesised as a potential nonpeptide mimic of somatostatin, based on conformational analysis of the endogenous ligand and molecular modelling studies. It displaced the radioligand [I-125-Tyr3]-octreotide with an IC50 of 23-mu-M.
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页码:135 / 140
页数:6
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