Synthesis of Phosphatase-stable, Cell-permeable Peptidomimetic Prodrugs That Target the SH2 Domain of Stat3

Overview

Journal Org Lett

Publisher American Chemical Society

Specialties Biochemistry
Chemistry

Date 2009 Jul 15

PMID 19594124

Citations 32

Authors

Pijus K Mandal

Warren S-L Liao

John S McMurray

Affiliations

Soon will be listed here.

Abstract

The synthesis of prodrugs targeted to the SH2 domain of Stat3 is reported. Using a convergent strategy, the pivaloyloxymethyl phosphonodiester of pentachlorophenyl 4-phosphonodifluoromethylcinnamate, a phosphotyrosine surrogate, was synthesized and used to acylate peptidomimetic fragments that were prepared on solid supports. Two prodrugs described here inhibited the phosphorylation of Stat3 in breast tumor cells.

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