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  • Title: Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.
    Author: Lu C, Tang K, Li Y, Li P, Lin Z, Yin D, Chen X, Huang H.
    Journal: Eur J Med Chem; 2014 Apr 22; 77():351-60. PubMed ID: 24675135.
    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.
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