Literature DB >> 15149680

Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.

Christopher G Barber1, Roger P Dickinson, Paul V Fish.   

Abstract

A series of 1-isoquinolinylguanidines are shown to be potent inhibitors of uPA with selectivity over tPA and plasmin. Potency is enhanced by the presence of a 4-halo and a 7-aryl substituent, particularly when substituted by a 3-carboxylic acid group. Compound 13j (UK-356,202) combines excellent potency and selectivity, and has been selected as a candidate for clinical evaluation.

Entities:  

Mesh:

Substances:

Year:  2004        PMID: 15149680     DOI: 10.1016/j.bmcl.2004.03.094

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


  8 in total

Review 1.  Drug development against metastasis-related genes and their pathways: a rationale for cancer therapy.

Authors:  Megumi Iiizumi; Wen Liu; Sudha K Pai; Eiji Furuta; Kounosuke Watabe
Journal:  Biochim Biophys Acta       Date:  2008-07-22

Review 2.  Green tea catechin, epigallocatechin-3-gallate (EGCG): mechanisms, perspectives and clinical applications.

Authors:  Brahma N Singh; Sharmila Shankar; Rakesh K Srivastava
Journal:  Biochem Pharmacol       Date:  2011-07-30       Impact factor: 5.858

3.  Discovery of novel urokinase plasminogen activator (uPA) inhibitors using ligand-based modeling and virtual screening followed by in vitro analysis.

Authors:  Mahmoud A Al-Sha'er; Mohammad A Khanfar; Mutasem O Taha
Journal:  J Mol Model       Date:  2014-01-28       Impact factor: 1.810

Review 4.  Urokinase plasminogen activator as an anti-metastasis target: inhibitor design principles, recent amiloride derivatives, and issues with human/mouse species selectivity.

Authors:  Nehad S El Salamouni; Benjamin J Buckley; Marie Ranson; Michael J Kelso; Haibo Yu
Journal:  Biophys Rev       Date:  2022-01-06

5.  Site-selective Suzuki-Miyaura coupling of heteroaryl halides - understanding the trends for pharmaceutically important classes.

Authors:  Joshua Almond-Thynne; David C Blakemore; David C Pryde; Alan C Spivey
Journal:  Chem Sci       Date:  2016-08-09       Impact factor: 9.825

6.  Uncharged isocoumarin-based inhibitors of urokinase-type plasminogen activator.

Authors:  Justin J Heynekamp; Lucy A Hunsaker; Thomas A Vander Jagt; Lorraine M Deck; David L Vander Jagt
Journal:  BMC Chem Biol       Date:  2006-02-08

7.  Application of molecular modeling to urokinase inhibitors development.

Authors:  V B Sulimov; E V Katkova; I V Oferkin; A V Sulimov; A N Romanov; A I Roschin; I B Beloglazova; O S Plekhanova; V A Tkachuk; V A Sadovnichiy
Journal:  Biomed Res Int       Date:  2014-05-20       Impact factor: 3.411

8.  Inhibitors of urokinase type plasminogen activator and cytostatic activity from crude plants extracts.

Authors:  Xueqiang Zha; Ricardo Diaz; Jose Javier Rosado Franco; Veronica Forbes Sanchez; Ezio Fasoli; Gabriel Barletta; Augusto Carvajal; Vibha Bansal
Journal:  Molecules       Date:  2013-07-26       Impact factor: 4.411

  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.