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Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.

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 K(i) value of 7.3 microM in a competitive fluorescence-polarization-based binding assay, representing a promising initial lead compound for further optimization.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Chen J,Nikolovska-Coleska Z,Yang CY,Gomez C,Gao W,Krajewski K,Jiang S,Roller P,Wang S

doi

10.1016/j.bmcl.2007.04.096

subject

Has Abstract

pub_date

2007-07-15 00:00:00

pages

3939-42

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(07)00526-4

journal_volume

17

pub_type

杂志文章

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