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

Jianyong Chen; Zaneta Nikolovska-Coleska; Chao Yie Yang; Cindy Gomez; Wei Gao; Krzysztof Krajewski; Sheng Jiang; Peter Roller; Shaomeng Wang

doi:10.1016/j.bmcl.2007.04.096

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

Jianyong Chen, Zaneta Nikolovska-Coleska, Chao Yie Yang, Cindy Gomez, Wei Gao, Krzysztof Krajewski, Sheng Jiang, Peter Roller, Shaomeng Wang

Research output: Contribution to journal › Article › peer-review

60 Scopus citations

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 μM in a competitive fluorescence-polarization-based binding assay, representing a promising initial lead compound for further optimization.

Original language	English
Pages (from-to)	3939-3942
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	17
Issue number	14
DOIs	https://doi.org/10.1016/j.bmcl.2007.04.096
State	Published - 15 Jul 2007
Externally published	Yes

Keywords

Click chemistry
Conformationally
Constrained mimetic
STAT3

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10.1016/j.bmcl.2007.04.096

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title = "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 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, Conformationally, Constrained mimetic, STAT3",

author = "Jianyong Chen and Zaneta Nikolovska-Coleska and Yang, \{Chao Yie\} and Cindy Gomez and Wei Gao and Krzysztof Krajewski and Sheng Jiang and Peter Roller and Shaomeng Wang",

year = "2007",

month = jul,

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doi = "10.1016/j.bmcl.2007.04.096",

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journal = "Bioorganic and Medicinal Chemistry Letters",

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TY - JOUR

T1 - Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'

AU - Chen, Jianyong

AU - Nikolovska-Coleska, Zaneta

AU - Yang, Chao Yie

AU - Gomez, Cindy

AU - Gao, Wei

AU - Krajewski, Krzysztof

AU - Jiang, Sheng

AU - Roller, Peter

AU - Wang, Shaomeng

PY - 2007/7/15

Y1 - 2007/7/15

N2 - 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.

AB - 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.

KW - Click chemistry

KW - Conformationally

KW - Constrained mimetic

KW - STAT3

UR - https://www.scopus.com/pages/publications/34250349898

U2 - 10.1016/j.bmcl.2007.04.096

DO - 10.1016/j.bmcl.2007.04.096

M3 - 文章

C2 - 17513110

AN - SCOPUS:34250349898

SN - 0960-894X

VL - 17

SP - 3939

EP - 3942

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 14

ER -

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

Abstract

Keywords

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