Literature DB >> 16134930

4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.

Lara S Kallander1, Qing Lu, Wenfang Chen, Thaddeus Tomaszek, Guang Yang, David Tew, Thomas D Meek, Glenn A Hofmann, Christina K Schulz-Pritchard, Ward W Smith, Cheryl A Janson, M Dominic Ryan, Gui-Feng Zhang, Kyung O Johanson, Robert B Kirkpatrick, Thau F Ho, Paul W Fisher, Michael R Mattern, Randall K Johnson, Michael J Hansbury, James D Winkler, Keith W Ward, Daniel F Veber, Scott K Thompson.   

Abstract

Inhibitors of human methionine aminopeptidase type 2 (hMetAP2) are of interest as potential treatments for cancer. A new class of small molecule reversible inhibitors of hMetAP2 was discovered and optimized, the 4-aryl-1,2,3-triazoles. Compound 24, a potent inhibitor of cobalt-activated hMetAP2, also inhibits human and mouse endothelial cell growth. Using a mouse matrigel model, this reversible hMetAP2 inhibitor was also shown to inhibit angiogenesis in vivo.

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Year:  2005        PMID: 16134930     DOI: 10.1021/jm050408c

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  13 in total

1.  Hot spot analysis for driving the development of hits into leads in fragment-based drug discovery.

Authors:  David R Hall; Chi Ho Ngan; Brandon S Zerbe; Dima Kozakov; Sandor Vajda
Journal:  J Chem Inf Model       Date:  2011-12-15       Impact factor: 4.956

Review 2.  Targeting Metalloenzymes for Therapeutic Intervention.

Authors:  Allie Y Chen; Rebecca N Adamek; Benjamin L Dick; Cy V Credille; Christine N Morrison; Seth M Cohen
Journal:  Chem Rev       Date:  2018-09-07       Impact factor: 60.622

Review 3.  Targeting the undruggable proteome: the small molecules of my dreams.

Authors:  Craig M Crews
Journal:  Chem Biol       Date:  2010-06-25

4.  Thrombospondin-1 inhibits nitric oxide signaling via CD36 by inhibiting myristic acid uptake.

Authors:  Jeff S Isenberg; Yifeng Jia; Julia Fukuyama; Christopher H Switzer; David A Wink; David D Roberts
Journal:  J Biol Chem       Date:  2007-04-05       Impact factor: 5.157

5.  Analyzing the binding of Co(II)-specific inhibitors to the methionyl aminopeptidases from Escherichia coli and Pyrococcus furiosus.

Authors:  Sanghamitra Mitra; George Sheppard; Jieyi Wang; Brian Bennett; Richard C Holz
Journal:  J Biol Inorg Chem       Date:  2009-02-06       Impact factor: 3.358

6.  Intercepting the Banert cascade with nucleophilic fluorine: direct access to α-fluorinated NH-1,2,3-triazoles.

Authors:  J R Alexander; P V Kevorkian; J J Topczewski
Journal:  Chem Commun (Camb)       Date:  2021-05-20       Impact factor: 6.222

7.  Potential inhibitors of methionine aminopeptidase type II identified via structure-based pharmacophore modeling.

Authors:  Safana Albayati; Abdullahi Ibrahim Uba; Kemal Yelekçi
Journal:  Mol Divers       Date:  2021-04-13       Impact factor: 2.943

8.  Silver Mediated Banert Cascade with Carbon Nucleophiles.

Authors:  Juliana R Alexander; Paul V Kevorkian; Joseph J Topczewski
Journal:  Org Lett       Date:  2021-04-02       Impact factor: 6.005

9.  Synthesis of Tris-Heterocycles via a Cascade IMCR/Aza Diels-Alder + CuAAC Strategy.

Authors:  Manuel A Rentería-Gómez; Alejandro Islas-Jácome; Shrikant G Pharande; David A Vosburg; Rocío Gámez-Montaño
Journal:  Front Chem       Date:  2019-08-06       Impact factor: 5.221

Review 10.  Metallo-aminopeptidase inhibitors.

Authors:  Artur Mucha; Marcin Drag; John P Dalton; Paweł Kafarski
Journal:  Biochimie       Date:  2010-05-10       Impact factor: 4.079

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