Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents
Compound C5 exhibited the most potent EGFR inhibitory activity with IC 50 of 0.07 μM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound C5 into the EGFR active site to determine the probable binding model. Besides, compound C5 showed signif...
Saved in:
Published in: | Bioorganic & medicinal chemistry 2010-07, Vol.18 (13), p.4606-4614 |
---|---|
Main Authors: | , , , , |
Format: | Article |
Language: | English |
Subjects: | |
Citations: | Items that this one cites Items that cite this one |
Online Access: | Get full text |
Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
Summary: | Compound
C5 exhibited the most potent EGFR inhibitory activity with IC
50 of 0.07
μM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound
C5 into the EGFR active site to determine the probable binding model. Besides, compound
C5 showed significant antiproliferative activity against MCF-7 with IC
50 of 0.08
μM, which would be a potential anticancer agent.
Two series of pyrazole derivatives designing for potential EGFR kinase inhibitors have been discovered. Some of them exhibited significant EGFR inhibitory activity. Compound
3-(3,4-dimethylphenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide (
C5) displayed the most potent EGFR inhibitory activity with IC
50 of 0.07
μM, which was comparable to the positive control erlotinib. Docking simulation was performed to position compound
C5 into the EGFR active site to determine the probable binding model. Antiproliferative assay results indicating that some of the pyrazole derivatives own high antiproliferative activity against MCF-7. Compound
C5 showed significant antiproliferative activity against MCF-7 with IC
50 of 0.08
μM. Therefore, compound
C5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent. |
---|---|
ISSN: | 0968-0896 1464-3391 |
DOI: | 10.1016/j.bmc.2010.05.034 |