FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2772902864> ?p ?o ?g. }

• W2772902864 endingPage "348" @default.
• W2772902864 startingPage "330" @default.
• W2772902864 abstract "Being responsible for the development of many cancer types, EGFR (Epidermal Growth Factor Receptor) and HER2 (Human Epidermal growth factor Receptor 2) were the focus of this study where a series of novel 4-anilino-furo[2,3-d]pyrimidine derivatives was designed, synthesized and biologically evaluated. Modification of the solvent accessible 5-position side chain greatly affected the in-vitro EGFR/HER2 inhibitory activity. Three derivatives bearing 5-carboxylic acid side chain, namely the 3-chloroanilino derivative (8c), the 3-bromoaniline (8d) and the lapatinib analogue (10) demonstrated the most significant submicromolar EGFR inhibition. Surprisingly, the in-vitro assay of the ester 7h and its acid analogue 10 showed a significant variation of results between the antiproliferative activity against A549 cell line (IC50 0.5 and 21.4 μM) respectively and EGFR inhibitory activity (18% and 100%) respectively, suggesting that 7h might be a prodrug for 10. This assumption was also affirmed by the in-vivo results, where the in-vivo antitumor assessment against EAC (Ehrlich Ascites Carcinoma) solid tumor model revealed that 7h and 8d (10 mg/kg dose) exhibited antitumor activity comparable to that of gefitinib at the same dose, exhibiting TGI% of 67%, 71% and 70%, respectively. This effect could be explained, at least partly, via activation of apoptosis, where 7h and 8d caused more than 2-fold increase of caspase 3 and cytochrome c expression than the control group which is comparable to that of gefitinib-treated group. Finally, 7h was the most effective apoptotic inducer, resulting in a significant elevation in annexin V–FITC-positive apoptotic cells (both early and late apoptosis) by 25 and 79-folds, respectively, compared to control, which is higher than that of gefitinib (22 and 61-folds, respectively)." @default.
• W2772902864 created "2017-12-22" @default.
• W2772902864 creator A5003776521 @default.
• W2772902864 creator A5015959877 @default.
• W2772902864 creator A5017054054 @default.
• W2772902864 creator A5033098246 @default.
• W2772902864 creator A5039240531 @default.
• W2772902864 creator A5048245581 @default.
• W2772902864 creator A5065536618 @default.
• W2772902864 date "2018-01-01" @default.
• W2772902864 modified "2023-10-15" @default.
• W2772902864 title "Discovery of anilino-furo[2,3- d ]pyrimidine derivatives as dual inhibitors of EGFR/HER2 tyrosine kinase and their anticancer activity" @default.
• W2772902864 cites W1983161601 @default.
• W2772902864 cites W1986547462 @default.
• W2772902864 cites W1987009448 @default.
• W2772902864 cites W1988700043 @default.
• W2772902864 cites W1988816704 @default.
• W2772902864 cites W1995242599 @default.
• W2772902864 cites W2002215779 @default.
• W2772902864 cites W2003717480 @default.
• W2772902864 cites W2008600118 @default.
• W2772902864 cites W2012915718 @default.
• W2772902864 cites W2034132952 @default.
• W2772902864 cites W2049274590 @default.
• W2772902864 cites W2055391916 @default.
• W2772902864 cites W2055903396 @default.
• W2772902864 cites W2059664977 @default.
• W2772902864 cites W2064422408 @default.
• W2772902864 cites W2076044105 @default.
• W2772902864 cites W2084086160 @default.
• W2772902864 cites W2088642987 @default.
• W2772902864 cites W2108520616 @default.
• W2772902864 cites W2108598528 @default.
• W2772902864 cites W2110478240 @default.
• W2772902864 cites W2114918609 @default.
• W2772902864 cites W2122028337 @default.
• W2772902864 cites W2131664752 @default.
• W2772902864 cites W2136701318 @default.
• W2772902864 cites W2138604360 @default.
• W2772902864 cites W2143859186 @default.
• W2772902864 cites W2146860018 @default.
• W2772902864 cites W2147793660 @default.
• W2772902864 cites W2153438736 @default.
• W2772902864 cites W2157824687 @default.
• W2772902864 cites W2162106505 @default.
• W2772902864 cites W2169560977 @default.
• W2772902864 cites W2219206020 @default.
• W2772902864 cites W2275046656 @default.
• W2772902864 cites W2288763477 @default.
• W2772902864 cites W2316784700 @default.
• W2772902864 cites W2340808473 @default.
• W2772902864 cites W2344420315 @default.
• W2772902864 cites W2951079533 @default.
• W2772902864 cites W4249526857 @default.
• W2772902864 cites W2120121422 @default.
• W2772902864 doi "https://doi.org/10.1016/j.ejmech.2017.12.022" @default.
• W2772902864 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/29275232" @default.
• W2772902864 hasPublicationYear "2018" @default.
• W2772902864 type Work @default.
• W2772902864 sameAs 2772902864 @default.
• W2772902864 citedByCount "28" @default.
• W2772902864 countsByYear W27729028642018 @default.
• W2772902864 countsByYear W27729028642019 @default.
• W2772902864 countsByYear W27729028642020 @default.
• W2772902864 countsByYear W27729028642021 @default.
• W2772902864 countsByYear W27729028642022 @default.
• W2772902864 countsByYear W27729028642023 @default.
• W2772902864 crossrefType "journal-article" @default.
• W2772902864 hasAuthorship W2772902864A5003776521 @default.
• W2772902864 hasAuthorship W2772902864A5015959877 @default.
• W2772902864 hasAuthorship W2772902864A5017054054 @default.
• W2772902864 hasAuthorship W2772902864A5033098246 @default.
• W2772902864 hasAuthorship W2772902864A5039240531 @default.
• W2772902864 hasAuthorship W2772902864A5048245581 @default.
• W2772902864 hasAuthorship W2772902864A5065536618 @default.
• W2772902864 hasConcept C108215921 @default.
• W2772902864 hasConcept C121608353 @default.
• W2772902864 hasConcept C126322002 @default.
• W2772902864 hasConcept C150903083 @default.
• W2772902864 hasConcept C170493617 @default.
• W2772902864 hasConcept C185592680 @default.
• W2772902864 hasConcept C190283241 @default.
• W2772902864 hasConcept C202751555 @default.
• W2772902864 hasConcept C207001950 @default.
• W2772902864 hasConcept C2777329042 @default.
• W2772902864 hasConcept C2777752497 @default.
• W2772902864 hasConcept C2779321679 @default.
• W2772902864 hasConcept C2779438470 @default.
• W2772902864 hasConcept C2779786085 @default.
• W2772902864 hasConcept C2780580887 @default.
• W2772902864 hasConcept C42362537 @default.
• W2772902864 hasConcept C530470458 @default.
• W2772902864 hasConcept C55493867 @default.
• W2772902864 hasConcept C71924100 @default.
• W2772902864 hasConcept C86803240 @default.
• W2772902864 hasConcept C98274493 @default.
• W2772902864 hasConceptScore W2772902864C108215921 @default.
• W2772902864 hasConceptScore W2772902864C121608353 @default.

• next