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New syntheses of tetrazolylmethylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors.

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HAL Id: inserm-00168682

https://www.hal.inserm.fr/inserm-00168682

Submitted on 30 Aug 2007

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New syntheses of tetrazolylmethylphenylalanine and

O-malonyltyrosine as pTyr mimetics for the design of

STAT3 dimerization inhibitors.

Jennifer Dourlat, Bruno Valentin, Wang-Qing Liu, Christiane Garbay

To cite this version:

Jennifer Dourlat, Bruno Valentin, Wang-Qing Liu, Christiane Garbay. New syntheses of tetrazolyl-methylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimeriza-tion inhibitors.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2007, 17 (14), pp.3943-6. �10.1016/j.bmcl.2007.04.107�. �inserm-00168682�

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New syntheses of tetrazolylmethylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors

Jennifer Dourlat, Bruno Valentin, Wang-Qing Liu and Christiane Garbay.

The novel syntheses of two pTyr mimetics, L-tetrazolylmethylphenylalanine (L-Tmp) and L-O-malonyltyrosine (L-OMT) are reported. Incorporation into a high affinity ligand of the STAT3 SH2 domain identified L-OMT as the first nonphosphorus pTyr mimetic reported so far against the STAT3 SH2 domain.

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