Literature DB >> 19131248

N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).

Martin Allan1, Sukhdev Manku, Eric Therrien, Natalie Nguyen, Sylvia Styhler, Marie-France Robert, Anne-Christine Goulet, Andrea J Petschner, Gabi Rahil, A Robert Macleod, Robert Déziel, Jeffrey M Besterman, Hannah Nguyen, Amal Wahhab.   

Abstract

A series of N-benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides targeting co-activator associated arginine methyltransferase 1 (CARM1) have been designed and synthesized. The potency of these inhibitors was influenced by the nature of the heteroaryl fragment with the thiophene analogues being superior to thiazole, pyridine, isoindoline and benzofuran based inhibitors.

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Year:  2008        PMID: 19131248     DOI: 10.1016/j.bmcl.2008.12.075

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


  26 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

2.  Effects of a novel arginine methyltransferase inhibitor on T-helper cell cytokine production.

Authors:  Kevin Bonham; Saskia Hemmers; Yeon-Hee Lim; Dawn M Hill; M G Finn; Kerri A Mowen
Journal:  FEBS J       Date:  2010-03-22       Impact factor: 5.542

Review 3.  Small Molecule Inhibitors of Protein Arginine Methyltransferases.

Authors:  Hao Hu; Kun Qian; Meng-Chiao Ho; Y George Zheng
Journal:  Expert Opin Investig Drugs       Date:  2016-02-16       Impact factor: 6.206

Review 4.  Chromatin proteins and modifications as drug targets.

Authors:  Kristian Helin; Dashyant Dhanak
Journal:  Nature       Date:  2013-10-24       Impact factor: 49.962

5.  Design and synthesis of selective, small molecule inhibitors of coactivator-associated arginine methyltransferase 1 (CARM1).

Authors:  H Ü Kaniskan; M S Eram; J Liu; D Smil; M L Martini; Y Shen; V Santhakumar; P J Brown; C Arrowsmith; M Vedadi; J Jin
Journal:  Medchemcomm       Date:  2016-07-13       Impact factor: 3.597

Review 6.  Protein methyltransferases as a target class for drug discovery.

Authors:  Robert A Copeland; Michael E Solomon; Victoria M Richon
Journal:  Nat Rev Drug Discov       Date:  2009-09       Impact factor: 84.694

Review 7.  Inhibitors of Protein Methyltransferases and Demethylases.

Authors:  H Ümit Kaniskan; Michael L Martini; Jian Jin
Journal:  Chem Rev       Date:  2017-03-24       Impact factor: 60.622

Review 8.  Recent progress in developing selective inhibitors of protein methyltransferases.

Authors:  H Ümit Kaniskan; Jian Jin
Journal:  Curr Opin Chem Biol       Date:  2017-06-26       Impact factor: 8.822

9.  Identification of small-molecule enhancers of arginine methylation catalyzed by coactivator-associated arginine methyltransferase 1.

Authors:  Sabrina Castellano; Astrid Spannhoff; Ciro Milite; Fabrizio Dal Piaz; Donghang Cheng; Alessandra Tosco; Monica Viviano; Abdellah Yamani; Agostino Cianciulli; Marina Sala; Vincent Cura; Jean Cavarelli; Ettore Novellino; Antonello Mai; Mark T Bedford; Gianluca Sbardella
Journal:  J Med Chem       Date:  2012-11-02       Impact factor: 7.446

10.  Exploiting an allosteric binding site of PRMT3 yields potent and selective inhibitors.

Authors:  Feng Liu; Fengling Li; Anqi Ma; Elena Dobrovetsky; Aiping Dong; Cen Gao; Ilia Korboukh; Jing Liu; David Smil; Peter J Brown; Stephen V Frye; Cheryl H Arrowsmith; Matthieu Schapira; Masoud Vedadi; Jian Jin
Journal:  J Med Chem       Date:  2013-02-27       Impact factor: 7.446

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