Literature DB >> 25288188

2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway.

Matthew G LaPorte1, Dimas José da Paz Lima2, Feng Zhang2, Malabika Sen3, Jennifer R Grandis4, Daniel Camarco5, Yun Hua5, Paul A Johnston6, John S Lazo7, Lynn O Resnick2, Peter Wipf8, Donna M Huryn9.   

Abstract

Synthesis and SAR investigation of 2-guanidinoquinazolines, initially identified in a high content screen for selective STAT3 pathway inhibitors, led to a more potent analog (11c) that demonstrated improved anti-proliferative activity against a panel of HNSCC cell lines.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Cancer cell line screening; Guanidinoquinazolines; STAT3 pathway; Skraup synthesis; Structure–activity relationships

Mesh：

Substances：

Year:  2014        PMID： 25288188      PMCID： PMC4250329          DOI： 10.1016/j.bmcl.2014.09.001

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


  26 in total

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Journal:  Cancer Biol Ther       Date:  2012-05-01       Impact factor: 4.742

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Journal:  Antimicrob Agents Chemother       Date:  2009-04-13       Impact factor: 5.191

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4.  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

5.  Novel small molecular inhibitors disrupt the JAK/STAT3 and FAK signaling pathways and exhibit a potent antitumor activity in glioma cells.

Authors:  Karolina Swiatek-Machado; Jakub Mieczkowski; Aleksandra Ellert-Miklaszewska; Piotr Swierk; Izabela Fokt; Slawomir Szymanski; Stanislaw Skora; Wiesław Szeja; Grzegorz Grynkiewicz; Bogdan Lesyng; Waldemar Priebe; Bozena Kaminska
Journal:  Cancer Biol Ther       Date:  2012-06-01       Impact factor: 4.742

6.  Quinazolin-2-ylamino-quinazolin-4-ols as novel non-nucleoside inhibitors of bacterial DNA polymerase III.

Authors:  Joseph Guiles; Xicheng Sun; Ian A Critchley; Urs Ochsner; Ming Tregay; Kim Stone; Jennifer Bertino; Louis Green; Rob Sabin; Frank Dean; H Garry Dallmann; Charles S McHenry; Nebojsa Janjic
Journal:  Bioorg Med Chem Lett       Date:  2008-12-13       Impact factor: 2.823

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Authors:  Douglas Hanahan; Robert A Weinberg
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Authors:  Thomas R Webb; Dmitriy Lvovskiy; Soon Ai Kim; Xiao duo Ji; Neli Melman; Joel Linden; Kenneth A Jacobson
Journal:  Bioorg Med Chem       Date:  2003-01-02       Impact factor: 3.641

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Authors:  Pol Specenier; Jan B Vermorken
Journal:  Biologics       Date:  2013-04-15

10.  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
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  5 in total

1.  HCS campaign to identify selective inhibitors of IL-6-induced STAT3 pathway activation in head and neck cancer cell lines.

Authors:  Paul A Johnston; Malabika Sen; Yun Hua; Daniel P Camarco; Tong Ying Shun; John S Lazo; Gabriela Mustata Wilson; Lynn O Resnick; Matthew G LaPorte; Peter Wipf; Donna M Huryn; Jennifer R Grandis
Journal:  Assay Drug Dev Technol       Date:  2015-09       Impact factor: 1.738

2.  New fluorescence-based high-throughput screening assay for small molecule inhibitors of tyrosyl-DNA phosphodiesterase 2 (TDP2).

Authors:  Carlos J A Ribeiro; Jayakanth Kankanala; Ke Shi; Kayo Kurahashi; Evgeny Kiselev; Azhar Ravji; Yves Pommier; Hideki Aihara; Zhengqiang Wang
Journal:  Eur J Pharm Sci       Date:  2018-03-21       Impact factor: 4.384

3.  Mechanism of action of selective inhibitors of IL-6 induced STAT3 pathway in head and neck cancer cell lines.

Authors:  Malabika Sen; Paul A Johnston; Netanya I Pollock; Kara DeGrave; Sonali C Joyce; Maria L Freilino; Yun Hua; Daniel P Camarco; David A Close; Donna M Huryn; Peter Wipf; Jennifer R Grandis
Journal:  J Chem Biol       Date:  2017-05-11

4.  Optimization of pyrazole-containing 1,2,4-triazolo-[3,4-b]thiadiazines, a new class of STAT3 pathway inhibitors.

Authors:  Matthew G LaPorte; Zhuzhu Wang; Raffaele Colombo; Atefeh Garzan; Vsevolod A Peshkov; Mary Liang; Paul A Johnston; Mark E Schurdak; Malabika Sen; Daniel P Camarco; Yun Hua; Netanya I Pollock; John S Lazo; Jennifer R Grandis; Peter Wipf; Donna M Huryn
Journal:  Bioorg Med Chem Lett       Date:  2016-06-09       Impact factor: 2.823

5.  Quinazoline Ligands Induce Cancer Cell Death through Selective STAT3 Inhibition and G-Quadruplex Stabilization.

Authors:  Jan Jamroskovic; Mara Doimo; Karam Chand; Ikenna Obi; Rajendra Kumar; Kristoffer Brännström; Mattias Hedenström; Rabindra Nath Das; Almaz Akhunzianov; Marco Deiana; Kazutoshi Kasho; Sebastian Sulis Sato; Parham L Pourbozorgi; James E Mason; Paolo Medini; Daniel Öhlund; Sjoerd Wanrooij; Erik Chorell; Nasim Sabouri
Journal:  J Am Chem Soc       Date:  2020-01-28       Impact factor: 15.419
  5 in total

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