期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 56, 期 3, 页码 1350-1354出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm301677r
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资金
- Dutch Technology Foundation STW
- Applied Science Division of NWO
- Technology Program of the Ministry of Economic Affairs
- Swedish Research Council [621-2009-5656, 621-2003-4265]
- European Community [HEALTH-F2-2011-256986]
Inhibitors for galectin-1 and -3 were synthesized from thiodigalactoside and lactosamine by derivatization of the galactose C3. Introduction of 4-phenyl-1H-1,2,3-triazol-1-yl substituents at the thiodigalactoside C3 by CuAAC, targeting arginine-arene interactions, increased the affinity to 13 nM but yielded little selectivity. The builder 4-(4-phenoxypheny1)-1H-1,2,3-triazol-1-yl substituent, however, increased the preference for galectin-3 over galectin-1 to more than 200-fold. Modeling showed more arginine-arene interactions for galectin-3 than for galectin-1. Introducing 4-phenoxyaryl groups on lactosamine had a similar effect.
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