Literature DB >> 21602043

Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.

Jan Kehler1, Andreas Ritzen, Morten Langgård, Sebastian Leth Petersen, Mohamed M Farah, Christoffer Bundgaard, Claus Tornby Christoffersen, Jacob Nielsen, John Paul Kilburn.   

Abstract

Novel triazoloquinazolines have been found as phosphodiesterase 10A (PDE10A) inhibitors. Structure-activity studies improved the initial micromolar potency which was found in the lead compound by a 100-fold identifying 5-(1H-benzoimidazol-2-ylmethylsulfanyl)-2-methyl-[1,2,4]triazolo[1,5-c]quinazoline, 42 (PDE10A IC(50)=12 nM) as the most potent compound from the series. Two X-ray structures revealed novel binding modes to the catalytic site of the PDE10A enzyme.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21602043     DOI： 10.1016/j.bmcl.2011.04.067

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


  6 in total

1.  Synthesis and Anticancer Activity of 2-(Alkyl-, Alkaryl-, Aryl-, Hetaryl-)-[1,2,4]triazolo[1,5-c]quinazolines.

Authors:  Sergiy I Kovalenko; Lyudmyla M Antypenko; Andriy K Bilyi; Sergiy V Kholodnyak; Olexandr V Karpenko; Olexii M Antypenko; Natalya S Mykhaylova; Tetyana I Los; Olexandra S Kolomoets
Journal:  Sci Pharm       Date:  2012-12-23

2.  Computer-aided design of multi-target ligands at A1R, A2AR and PDE10A, key proteins in neurodegenerative diseases.

Authors:  Leen Kalash; Cristina Val; Jhonny Azuaje; María I Loza; Fredrik Svensson; Azedine Zoufir; Lewis Mervin; Graham Ladds; José Brea; Robert Glen; Eddy Sotelo; Andreas Bender
Journal:  J Cheminform       Date:  2017-12-30       Impact factor: 5.514

3.  Structure-based identification of dual ligands at the A2AR and PDE10A with anti-proliferative effects in lung cancer cell-lines.

Authors:  Leen Kalash; Ian Winfield; Dewi Safitri; Marcel Bermudez; Sabrina Carvalho; Robert Glen; Graham Ladds; Andreas Bender
Journal:  J Cheminform       Date:  2021-03-03       Impact factor: 5.514

4.  Identification and Localization of the Cyclic Nucleotide Phosphodiesterase 10A in Bovine Testis and Mature Spermatozoa.

Authors:  Serge Goupil; Loïze Maréchal; Hassan El Hajj; Marie-Ève Tremblay; François J Richard; Pierre Leclerc
Journal:  PLoS One       Date:  2016-08-22       Impact factor: 3.240

5.  Phosphodiesterase 10A is overexpressed in lung tumor cells and inhibitors selectively suppress growth by blocking β-catenin and MAPK signaling.

Authors:  Bing Zhu; Ashley Lindsey; Nan Li; Kevin Lee; Veronica Ramirez-Alcantara; Joshua C Canzoneri; Alexandra Fajardo; Luciana Madeira da Silva; Meagan Thomas; John T Piazza; Larry Yet; Brian T Eberhardt; Evrim Gurpinar; Dennis Otali; William Grizzle; Jacob Valiyaveettil; Xi Chen; Adam B Keeton; Gary A Piazza
Journal:  Oncotarget       Date:  2017-08-27

6.  Impact of N-Alkylamino Substituents on Serotonin Receptor (5-HTR) Affinity and Phosphodiesterase 10A (PDE10A) Inhibition of Isoindole-1,3-dione Derivatives.

Authors:  Anna Czopek; Anna Partyka; Adam Bucki; Maciej Pawłowski; Marcin Kołaczkowski; Agata Siwek; Monika Głuch-Lutwin; Paulina Koczurkiewicz; Elżbieta Pękala; Anna Jaromin; Bożena Tyliszczak; Anna Wesołowska; Agnieszka Zagórska
Journal:  Molecules       Date:  2020-08-25       Impact factor: 4.411
  6 in total

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