Literature DB >> 19243938

Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors.

Cindy Gomez1, Longchuan Bai, Jian Zhang, Zaneta Nikolovska-Coleska, Jianyong Chen, Han Yi, Shaomeng Wang.   

Abstract

The STAT3 oncogene is a promising molecular target for the design of a new class of anticancer drugs. In this letter, we describe the design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as novel STAT3 inhibitors. Compound 3 binds to STAT3 with a K(i) value of 190nM and is a promising lead compound for further design and optimization.

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Year:  2009        PMID: 19243938     DOI: 10.1016/j.bmcl.2009.01.091

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


  8 in total

1.  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

2.  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

3.  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

4.  Structure-affinity relationships of glutamine mimics incorporated into phosphopeptides targeted to the SH2 domain of signal transducer and activator of transcription 3.

Authors:  Pijus K Mandal; Zhiyong Ren; Xiaomin Chen; Chiyi Xiong; John S McMurray
Journal:  J Med Chem       Date:  2009-10-08       Impact factor: 7.446

5.  Novel STAT3 small-molecule inhibitors identified by structure-based virtual ligand screening incorporating SH2 domain flexibility.

Authors:  Ren Kong; Uddalak Bharadwaj; T Kris Eckols; Mikhail Kolosov; Haoyi Wu; Francisco J Santa Cruz-Pavlovich; Alison Shaw; Oluwatomilona I Ifelayo; Hong Zhao; Moses M Kasembeli; Stephen T C Wong; David J Tweardy
Journal:  Pharmacol Res       Date:  2021-04-29       Impact factor: 10.334

6.  A natural product-like JAK2/STAT3 inhibitor induces apoptosis of malignant melanoma cells.

Authors:  Ke-Jia Wu; Jie-Min Huang; Hai-Jing Zhong; Zhen-Zhen Dong; Kasipandi Vellaisamy; Jin-Jian Lu; Xiu-Ping Chen; Pauline Chiu; Daniel W J Kwong; Quan-Bin Han; Dik-Lung Ma; Chung-Hang Leung
Journal:  PLoS One       Date:  2017-06-01       Impact factor: 3.240

7.  Critical analysis of the potential for targeting STAT3 in human malignancy.

Authors:  Noah D Peyser; Jennifer R Grandis
Journal:  Onco Targets Ther       Date:  2013-07-30       Impact factor: 4.147

Review 8.  STAT inhibitors for cancer therapy.

Authors:  Muhammad Furqan; Akintunde Akinleye; Nikhil Mukhi; Varun Mittal; Yamei Chen; Delong Liu
Journal:  J Hematol Oncol       Date:  2013-12-05       Impact factor: 17.388

  8 in total

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