Literature DB >> 22560627

2-Anilino-4-(benzimidazol-2-yl)pyrimidines--a multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines.

Renate Determann1, Jan Dreher, Knut Baumann, Lutz Preu, Peter G Jones, Frank Totzke, Christoph Schächtele, Michael H G Kubbutat, Conrad Kunick.   

Abstract

2-Anilino-4-(benzimidazol-2-yl)-pyrimidines, synthesized by reaction of a readily available benzimidazole-substituted enaminone with suitable arylguanidines, were shown to inhibit four cancer-related protein kinases (Aurora B, PLK1, FAK, and VEGF-R2). The most potent derivative exhibited antiproliferative activity for several cancer cell lines of the NCI in vitro cell line panel in submicromolar concentrations. Both the anilinopyrimidine structure and the substitution pattern at the aniline ring appear to be important for the protein kinase inhibitory activity.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.

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Year:  2012        PMID: 22560627     DOI: 10.1016/j.ejmech.2012.04.007

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Synthesis of Morpholine-, Piperidine-, and N-Substituted Piperazine-Coupled 2-(Benzimidazol-2-yl)-3-arylquinoxalines as Novel Potent Antitumor Agents.

Authors:  Vakhid A Mamedov; Nataliya A Zhukova; Alexandra D Voloshina; Victor V Syakaev; Tat'yana N Beschastnova; Anna P Lyubina; Syumbelya K Amerhanova; Aida I Samigullina; Aidar T Gubaidullin; Daina N Buzyurova; Il Dar Kh Rizvanov; Oleg G Sinyashin
Journal:  ACS Pharmacol Transl Sci       Date:  2022-09-01

2.  Microwave-assisted simple synthesis of 2-anilinopyrimidines by the reaction of 2-chloro-4,6-dimethylpyrimidine with aniline derivatives.

Authors:  Cristina Campestre; György Keglevich; János Kóti; Luca Scotti; Carla Gasbarri; Guido Angelini
Journal:  RSC Adv       Date:  2020-03-25       Impact factor: 3.361

Review 3.  FAK inhibitors as promising anticancer targets: present and future directions.

Authors:  Muhamad Mustafa; Amer Ali Abd El-Hafeez; Dalia A Abdelhafeez; Dalia Abdelhamid; Yaser A Mostafa; Pradipta Ghosh; Alaa M Hayallah; Gamal El-Din A Abuo-Rahma
Journal:  Future Med Chem       Date:  2021-08-03       Impact factor: 4.767

  3 in total

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