| Literature DB >> 24675135 |
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.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