Title of article
Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via ‘click chemistry’
Author/Authors
Jianyong Chen، نويسنده , , Zaneta Nikolovska-Coleska، نويسنده , , Chao-Yie Yang، نويسنده , , Cindy Gomez، نويسنده , , Wei Gao، نويسنده , , Krzysztof Krajewski، نويسنده , , Sheng Jiang، نويسنده , , Peter Roller، نويسنده , , Shaomeng Wang، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
3939
To page
3942
Abstract
STAT3 is a promising molecular target for the design of new anticancer drugs. In this paper, we report the design and synthesis of a conformationally constrained macrocyclic peptidomimetic 2 via click chemistry. Compound 2 was determined to bind to STAT3 with a Ki value of 7.3 μM in a competitive fluorescence-polarization-based binding assay, representing a promising initial lead compound for further optimization.
Keywords
click chemistry , Constrained mimetic , Conformationally , STAT3
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798343
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