Matches in SemOpenAlex for { <https://semopenalex.org/work/W2158933105> ?p ?o ?g. }
- W2158933105 endingPage "144" @default.
- W2158933105 startingPage "110" @default.
- W2158933105 abstract "A series of 1,2,3-triazole-containing Sorafenib analogues, in which the aryl urea moiety of Sorafenib (1) was replaced with a 1,2,3-triazole ring linking a substituted phenoxy fragment, were prepared successfully via Huisgen 1,3-dipolar cycloaddition and nucleophilic aromatic substitution. The studies of cytotoxicity towards human hepatocellular carcinoma (HCC) cell lines, HepG2 and Huh7, indicated that p-tert-butylphenoxy analogue 2m showed significant inhibitory activity against Huh7 with IC50 = 5.67 ± 0.57 µM. More importantly, 2m showed low cytotoxicity against human embryonal lung fibroblast cell line, MRC-5, with IC50 > 100 µM, suggesting its highly selective cytotoxic activity (SI > 17.6) towards Huh7 which is much superior to that of Sorafenib (SI = 6.73). The molecular docking studies revealed that the analogue 2m bound B-RAF near the binding position of Sorafenib, while it interacted VEGFR2 efficiently at the same binding position of Sorafenib. However, 2m exhibited moderate inhibitory activity toward B-RAF, implying that its anti-Huh7 effect might not strictly relate to inhibition of B-RAF. Wound healing and BrdU cell proliferation assays confirmed anti-cell migration and anti-cell proliferative activities towards Huh7. With its inhibitory efficiency and high safety profile, 2m has been identified as a promising candidate for the treatment of HCC." @default.
- W2158933105 created "2016-06-24" @default.
- W2158933105 creator A5003847273 @default.
- W2158933105 creator A5036220598 @default.
- W2158933105 creator A5041200743 @default.
- W2158933105 date "2013-05-01" @default.
- W2158933105 modified "2023-09-30" @default.
- W2158933105 title "United States Food and Drug Administration approved oral kinase inhibitors for the treatment of malignancies" @default.
- W2158933105 cites W1965429870 @default.
- W2158933105 cites W1968996549 @default.
- W2158933105 cites W1970687736 @default.
- W2158933105 cites W1971837077 @default.
- W2158933105 cites W1986095564 @default.
- W2158933105 cites W2023952988 @default.
- W2158933105 cites W2028959752 @default.
- W2158933105 cites W2030205108 @default.
- W2158933105 cites W2050249255 @default.
- W2158933105 cites W2055613955 @default.
- W2158933105 cites W2060105258 @default.
- W2158933105 cites W2061440903 @default.
- W2158933105 cites W2067216473 @default.
- W2158933105 cites W2097698108 @default.
- W2158933105 cites W2097799776 @default.
- W2158933105 cites W2099088585 @default.
- W2158933105 cites W2100912832 @default.
- W2158933105 cites W2101616608 @default.
- W2158933105 cites W2101776780 @default.
- W2158933105 cites W2110444464 @default.
- W2158933105 cites W2110835998 @default.
- W2158933105 cites W2111662961 @default.
- W2158933105 cites W2115351357 @default.
- W2158933105 cites W2115626434 @default.
- W2158933105 cites W2119358583 @default.
- W2158933105 cites W2119501407 @default.
- W2158933105 cites W2121743767 @default.
- W2158933105 cites W2127101185 @default.
- W2158933105 cites W2128542677 @default.
- W2158933105 cites W2129931005 @default.
- W2158933105 cites W2134787029 @default.
- W2158933105 cites W2135192471 @default.
- W2158933105 cites W2138297714 @default.
- W2158933105 cites W2139511378 @default.
- W2158933105 cites W2143006986 @default.
- W2158933105 cites W2147834058 @default.
- W2158933105 cites W2148012276 @default.
- W2158933105 cites W2148479421 @default.
- W2158933105 cites W2153477391 @default.
- W2158933105 cites W2155319477 @default.
- W2158933105 cites W2157262448 @default.
- W2158933105 cites W2158134441 @default.
- W2158933105 cites W2158269380 @default.
- W2158933105 cites W2158474413 @default.
- W2158933105 cites W2162424705 @default.
- W2158933105 cites W2165651085 @default.
- W2158933105 cites W2165837347 @default.
- W2158933105 cites W2166084034 @default.
- W2158933105 cites W2167903658 @default.
- W2158933105 cites W2169363650 @default.
- W2158933105 cites W2253507027 @default.
- W2158933105 cites W2328208895 @default.
- W2158933105 cites W2336907646 @default.
- W2158933105 cites W4238208852 @default.
- W2158933105 cites W4250769897 @default.
- W2158933105 doi "https://doi.org/10.1016/j.currproblcancer.2013.06.001" @default.
- W2158933105 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3761410" @default.
- W2158933105 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/23972982" @default.
- W2158933105 hasPublicationYear "2013" @default.
- W2158933105 type Work @default.
- W2158933105 sameAs 2158933105 @default.
- W2158933105 citedByCount "50" @default.
- W2158933105 countsByYear W21589331052013 @default.
- W2158933105 countsByYear W21589331052014 @default.
- W2158933105 countsByYear W21589331052015 @default.
- W2158933105 countsByYear W21589331052016 @default.
- W2158933105 countsByYear W21589331052017 @default.
- W2158933105 countsByYear W21589331052018 @default.
- W2158933105 countsByYear W21589331052019 @default.
- W2158933105 countsByYear W21589331052020 @default.
- W2158933105 countsByYear W21589331052021 @default.
- W2158933105 countsByYear W21589331052022 @default.
- W2158933105 countsByYear W21589331052023 @default.
- W2158933105 crossrefType "journal-article" @default.
- W2158933105 hasAuthorship W2158933105A5003847273 @default.
- W2158933105 hasAuthorship W2158933105A5036220598 @default.
- W2158933105 hasAuthorship W2158933105A5041200743 @default.
- W2158933105 hasBestOaLocation W21589331052 @default.
- W2158933105 hasConcept C109316439 @default.
- W2158933105 hasConcept C159110408 @default.
- W2158933105 hasConcept C185592680 @default.
- W2158933105 hasConcept C202751555 @default.
- W2158933105 hasConcept C2777752497 @default.
- W2158933105 hasConcept C2778019345 @default.
- W2158933105 hasConcept C2778695046 @default.
- W2158933105 hasConcept C41685203 @default.
- W2158933105 hasConcept C502942594 @default.
- W2158933105 hasConcept C54355233 @default.
- W2158933105 hasConcept C55493867 @default.
- W2158933105 hasConcept C62112901 @default.