Literature DB >> 17513110

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

Jianyong Chen1, Zaneta Nikolovska-Coleska, Chao-Yie Yang, Cindy Gomez, Wei Gao, Krzysztof Krajewski, Sheng Jiang, Peter Roller, Shaomeng Wang.   

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.

Entities:  

Mesh：

Substances：

Year:  2007        PMID： 17513110     DOI： 10.1016/j.bmcl.2007.04.096

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  22 in total

1.  Conformationally constrained peptidomimetic inhibitors of signal transducer and activator of transcription. 3: Evaluation and molecular modeling.

Authors:  Pijus K Mandal; Donald Limbrick; David R Coleman; Garrett A Dyer; Zhiyong Ren; J Sanderson Birtwistle; Chiyi Xiong; Xiaomin Chen; James M Briggs; John S McMurray
Journal:  J Med Chem       Date:  2009-04-23       Impact factor: 7.446

2.  Structure-Based Design of Conformationally Constrained, Cell-Permeable STAT3 Inhibitors.

Authors:  Jianyong Chen; Longchuan Bai; Denzil Bernard; Zaneta Nikolovska-Coleska; Cindy Gomez; Jian Zhang; Han Yi; Shaomeng Wang
Journal:  ACS Med Chem Lett       Date:  2010-05-13       Impact factor: 4.345

3.  Antagonism of the Stat3-Stat3 protein dimer with salicylic acid based small molecules.

Authors:  Steven Fletcher; Brent D G Page; Xialoei Zhang; Peibin Yue; Zhi Hua Li; Sumaiya Sharmeen; Jagdeep Singh; Wei Zhao; Aaron D Schimmer; Suzanne Trudel; James Turkson; Patrick T Gunning
Journal:  ChemMedChem       Date:  2011-05-25       Impact factor: 3.466

4.  Potent and selective phosphopeptide mimetic prodrugs targeted to the Src homology 2 (SH2) domain of signal transducer and activator of transcription 3.

Authors:  Pijus K Mandal; Fengqin Gao; Zhen Lu; Zhiyong Ren; Rajagopal Ramesh; J Sanderson Birtwistle; Kumaralal K Kaluarachchi; Xiaomin Chen; Robert C Bast; Warren S Liao; John S McMurray
Journal:  J Med Chem       Date:  2011-04-26       Impact factor: 7.446

5.  Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.

Authors:  Xiaomei Ren; Lei Duan; Qiang He; Zhang Zhang; Yi Zhou; Donghai Wu; Jingxuan Pan; Duanqing Pei; Ke Ding
Journal:  ACS Med Chem Lett       Date:  2010-09-07       Impact factor: 4.345

6.  Linker Variation and Structure-Activity Relationship Analyses of Carboxylic Acid-based Small Molecule STAT3 Inhibitors.

Authors:  Francisco Lopez-Tapia; Christine Brotherton-Pleiss; Peibin Yue; Heide Murakami; Ana Carolina Costa Araujo; Bruna Reis Dos Santos; Erin Ichinotsubo; Anna Rabkin; Raj Shah; Megan Lantz; Suzie Chen; Marcus A Tius; James Turkson
Journal:  ACS Med Chem Lett       Date:  2018-02-16       Impact factor: 4.345

7.  A phosphopeptide mimetic prodrug targeting the SH2 domain of Stat3 inhibits tumor growth and angiogenesis.

Authors:  Edmond J Auzenne; Jim Klostergaard; Pijus K Mandal; Warren S Liao; Zhen Lu; Fengqin Gao; Robert C Bast; Fredika M Robertson; John S McMurray
Journal:  J Exp Ther Oncol       Date:  2012

8.  Hirsutinolide Series Inhibit Stat3 Activity, Alter GCN1, MAP1B, Hsp105, G6PD, Vimentin, TrxR1, and Importin α-2 Expression, and Induce Antitumor Effects against Human Glioma.

Authors:  Gabriella Miklossy; Ui Joung Youn; Peibin Yue; Mingming Zhang; Chih-Hong Chen; Tyvette S Hilliard; David Paladino; Yifei Li; Justin Choi; Jann N Sarkaria; Joel K Kawakami; Supakit Wongwiwatthananukit; Yuan Chen; Dianqing Sun; Leng Chee Chang; James Turkson
Journal:  J Med Chem       Date:  2015-09-17       Impact factor: 7.446

Review 9.  Molecular approaches towards the inhibition of the signal transducer and activator of transcription 3 (Stat3) protein.

Authors:  Steven Fletcher; James Turkson; Patrick T Gunning
Journal:  ChemMedChem       Date:  2008-08       Impact factor: 3.466

10.  Disruption of transcriptionally active Stat3 dimers with non-phosphorylated, salicylic acid-based small molecules: potent in vitro and tumor cell activities.

Authors:  Steven Fletcher; Jagdeep Singh; Xiaolei Zhang; Peibin Yue; Brent D G Page; Sumaiya Sharmeen; Vijay M Shahani; Wei Zhao; Aaron D Schimmer; James Turkson; Patrick T Gunning
Journal:  Chembiochem       Date:  2009-08-17       Impact factor: 3.164
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.