Literature DB >> 19217288

Synthesis and structure-activity relationships of novel benzofuran farnesyltransferase inhibitors.

Kohsuke Asoh1, Masami Kohchi, Ikumi Hyoudoh, Tatsuo Ohtsuka, Miyako Masubuchi, Kenichi Kawasaki, Hirosato Ebiike, Yasuhiko Shiratori, Takaaki A Fukami, Osamu Kondoh, Toshiyuki Tsukaguchi, Nobuya Ishii, Yuko Aoki, Nobuo Shimma, Masahiro Sakaitani.   

Abstract

A series of benzofuran-based farnesyltransferase inhibitors have been designed and synthesized as antitumor agents. Among them, 11f showed the most potent enzyme inhibitory activity (IC(50)=1.1nM) and antitumor activity in human cancer xenografts in mice.

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Year:  2009        PMID： 19217288     DOI： 10.1016/j.bmcl.2009.01.074

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


  5 in total

1.  Tipifarnib-induced apoptosis in acute myeloid leukemia and multiple myeloma cells depends on Ca2+ influx through plasma membrane Ca2+ channels.

Authors:  Niranjan Yanamandra; Robert W Buzzeo; Mark Gabriel; Lori A Hazlehurst; Yelenis Mari; Darrin M Beaupre; Javier Cuevas
Journal:  J Pharmacol Exp Ther       Date:  2011-03-04       Impact factor: 4.030

2.  Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines.

Authors:  Saeed Ghasemi; Soodabeh Davaran; Simin Sharifi; Davoud Asgari; Ali Abdollahi; Javid Shahbazi Mojarrad
Journal:  Adv Pharm Bull       Date:  2013-02-07

3.  On the importance of composite protein multiple ligand interactions in protein pockets.

Authors:  Sam Tonddast-Navaei; Bharath Srinivasan; Jeffrey Skolnick
Journal:  J Comput Chem       Date:  2016-11-16       Impact factor: 3.376

4.  Structure-based design and synthesis of potent, ethylenediamine-based, mammalian farnesyltransferase inhibitors as anticancer agents.

Authors:  Steven Fletcher; Erin Pusateri Keaney; Christopher G Cummings; Michelle A Blaskovich; Michael A Hast; Matthew P Glenn; Sung-Youn Chang; Cynthia J Bucher; Ryan J Floyd; William P Katt; Michael H Gelb; Wesley C Van Voorhis; Lorena S Beese; Said M Sebti; Andrew D Hamilton
Journal:  J Med Chem       Date:  2010-10-14       Impact factor: 7.446

5.  Study of the cytotoxic/toxic potential of the novel anticancer selenodiazoloquinolone on fibroblast cells and 3D skin model.

Authors:  Soňa Jantová; Dominika Topoľská; Michaela Janošková; Miroslav Pánik; Viktor Milata
Journal:  Interdiscip Toxicol       Date:  2017-05-17
  5 in total

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