Abstract
The efficient construction of triazolyl peptidomimetics via the powerful click chemistry for the discovery of small molecule-based chemotherapeutic agents represents a promising strategy in drug development today. Herein, the synthesis of novel mono-triazolyl or bis-triazolyl amino acid derivatives was rapidly achieved via microwave-assisted Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition (CuAAC). Subsequent in vitro enzymatic assay on several homologous protein tyrosine phosphatases (PTPs) identified the triazolyl dimers as new specific inhibitors of Cell Cycle Division 25B (CDC25B) phosphatase and Protein Tyrosine Phosphatase 1B (PTP1B).
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