Journal
MOLECULES
Volume 21, Issue 11, Pages -Publisher
MDPI AG
DOI: 10.3390/molecules21111572
Keywords
diaryl urea; 4-aminoquinazolinyl; synthesis; cytotoxicity; EGFR inhibitors
Funding
- National Natural Science Foundation of China [21002065]
- Project of Education Department of Liaoning [L2013382]
- Development Project of Ministry of Education Innovation Team [IRT1073]
- Science and Technology Program of Shenyang [F15-139-9-02]
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Two novel series of diaryl urea derivatives 5a-i and 13a-l were synthesized and evaluated for their cytotoxicity against H-460, HT-29, A549, and MDA-MB-231 cancer cell lines in vitro. Therein, 4-aminoquinazolinyl-diaryl urea derivatives 5a-i demonstrated significant activity, and seven of them are more active than sorafenib, with IC50 values ranging from 0.089 to 5.46 mu M. Especially, compound 5a exhibited the most active potency both in cellular (IC50 = 0.15, 0.089, 0.36, and 0.75 mu M, respectively) and enzymatic assay (IC50 = 56 nM against EGFR), representing a promising lead for further optimization.
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