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Click Synthesis of Triazolyl Phenylalaninyl and Tyrosinyl Derivatives as New Protein Tyrosine Phosphatase Inhibitors
Author(s) -
Cui Lei,
He XiaoPeng,
Gao LiXin,
Li Jia,
Chen GuoRong
Publication year - 2013
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.1517
Subject(s) - chemistry , protein tyrosine phosphatase , click chemistry , tyrosine , combinatorial chemistry , phosphatase , biochemistry , stereochemistry , enzyme
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).