Literature DB >> 24675135

Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.

Chenshu Lu1, Ke Tang1, Yan Li1, Peng Li1, Ziyun Lin1, Dali Yin1, Xiaoguang Chen2, Haihong Huang3.   

Abstract

A novel series of diaryl ureas containing different linker groups were designed and synthesized. Their in vitro antitumor activity against MX-1, A375, HepG2, Ketr3 and HT-29 was evaluated using the standard MTT assay. Compounds having a rigid linker group such as vinyl, ethynyl and phenyl showed significant inhibitory activity against a variety of cancer cell lines. Specifically, compound 23 with a phenyl linker group demonstrated broad-spectrum antitumor activity with IC50 values of 5.17-6.46 μM against five tested tumor cell lines. Compound 23 is more potent than reference drug sorafenib (8.27-15.2 μM), representing a promising lead for further optimization.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Antitumor activity; Diaryl ureas; Linker; Sorafenib

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Year:  2014        PMID: 24675135     DOI: 10.1016/j.ejmech.2014.03.020

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


  2 in total

1.  Design, Synthesis and Evaluation of the Biological Activities of Some New Carbohydrazide and Urea Derivatives.

Authors:  Fatih Tok; Recep Ilhan; Selin Günal; Petek Ballar-Kirmizibayrak; Bedia Koçyiğit-Kaymakçioğlu
Journal:  Turk J Pharm Sci       Date:  2018-11-20

2.  Synthesis and biological evaluation of a new series of 1-aryl-3-[4-(pyridin-2-ylmethoxy)phenyl]urea derivatives as new anticancer agents.

Authors:  Jian Feng; Tai Li; Shishao Liang; Chuanming Zhang; Xiaoyu Tan; Ning Ding; Xin Wang; Xiaoping Liu; Chun Hu
Journal:  Med Chem Res       Date:  2020-05-18       Impact factor: 1.965

  2 in total

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