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Abstract
Cellular mesenchymal-epithelial transition factor (c-MET) is closely linked to human malignancies, which makes it an important target for treatment of cancer. In this study, a series of 3-methoxy-N-phenylbenzamide derivatives, N-(3-(tert-butyl)-1-phenyl-1H-pyrazol-5-yl) benzamide derivatives and N1-(3-fluoro-4-methoxyphenyl)-N3-(4-fluorophenyl) malonamide derivatives were designed and synthesized, some of them were identified as c-MET inhibitors. Among these compounds with new scaffolds having different quinazoline, pyridine and tetrahydro-pyridothienopyrimidine head groups, compound 11c, 11i, 13b, 13h exhibited both potent inhibitory activities against c-MET and high anticancer activity against tested cancer cell lines in vitro. In addition, kinase selectivity assay further demonstrated that both 13b and 13h are potent and selective c-MET inhibitors. Molecular docking supported that they bound well to c-MET and VEGFR2, which demonstrates that they are potential c-MET RTK inhibitors for cancer therapy.
Highlights
IntroductionTyrosine kinase phosphate group group from from ATPATP to Tyrosine kinase is is an an enzyme enzyme that that transfers transfers aa phosphate to aa protein, protein, and and it it functions as an “on” or “off”switch in many cellular functions.They become potent oncogene that functions as an “on” or “off” switch in many cellular functions
Tyrosine kinase is is an an enzyme enzyme that that transfers transfers aa phosphate to aa protein, protein, and and it it functions as an switch in many cellular functions
The chemistry described in Scheme 1 shows the synthetic route chosen to obtain quinazolines (Compound 5), pyridines (Compound 6) and tetrahydro-pyridothienopyrimidines (Compound 7)
Summary
ATP to Tyrosine kinase is is an an enzyme enzyme that that transfers transfers aa phosphate to aa protein, protein, and and it it functions as an “on” or “off”. They become potent oncogene that functions as an “on” or “off” switch in many cellular functions They become potent oncogene that has the the potential potential to to cause cause cancer, cancer, when. Several has when they they are are often often mutated mutated or or expressed expressed at at high high levels levels [1]. Several receptor tyrosine have effective effective anti-tumor anti-tumor activity activity and and receptor tyrosine kinases kinases (RTKs). (RTKs) inhibitors inhibitors have have been been found found to to have some of them have been approved or are in clinical trials.
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