FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2003392551> ?p ?o ?g. }

• W2003392551 endingPage "162" @default.
• W2003392551 startingPage "153" @default.
• W2003392551 abstract "To potentiate the quinazoline-based inhibitor of the epidermal growth factor receptor (EGFR), a chloroethyl alkylating moiety was appended to its 6-position. This led to molecules with extremely strong EGFR inhibitory potency and anomalously strong DNA-damaging potential. To assess the role of the chloroethyl group on potency, we designed a molecule in which it is shifted to the 7-position where it would be less reactive and away from the cys773 of the EGFR ATP site. The results showed that (i) ZR2009 was 10-fold less potent than its positional isomer ZR2003 in EGFR tyrosine kinase inhibition, (ii) it consistently exhibited significantly weaker antiproliferative potency than ZR2003, (iii) in reversibility assays, while ZR2003 induced sustained inhibition of EGFR phosphorylation, ZR2009 inhibitory activity was partially reversed, and (iv) likewise, ZR2009 significantly lost its activity in short exposure growth inhibitory assays and induced lower levels of DNA damage than ZR2003. Molecular modeling suggested that while the chloroethylamino group in ZR2003 was at 3.5 Å away from Cys773, that of ZR2009 was at 6.3 Å. The results in toto suggest that, while the chloroethyl is a strong alkylating group, its appendage to the 6-position is optimal for DNA damage, sustained EGFR, and growth inhibition." @default.
• W2003392551 created "2016-06-24" @default.
• W2003392551 creator A5003594028 @default.
• W2003392551 creator A5005009665 @default.
• W2003392551 creator A5036446709 @default.
• W2003392551 creator A5056074050 @default.
• W2003392551 creator A5078156446 @default.
• W2003392551 creator A5080076598 @default.
• W2003392551 date "2014-09-25" @default.
• W2003392551 modified "2023-09-24" @default.
• W2003392551 title "Positional Isomerization of A Non-Cleavable Combi-Molecule Dramatically Altered Tumor Cell Response Profile" @default.
• W2003392551 cites W1974903851 @default.
• W2003392551 cites W1977332018 @default.
• W2003392551 cites W1983005412 @default.
• W2003392551 cites W1986792926 @default.
• W2003392551 cites W1993969876 @default.
• W2003392551 cites W1995242599 @default.
• W2003392551 cites W2001276579 @default.
• W2003392551 cites W2004326614 @default.
• W2003392551 cites W2007649418 @default.
• W2003392551 cites W2011446012 @default.
• W2003392551 cites W2016469173 @default.
• W2003392551 cites W2022039302 @default.
• W2003392551 cites W2027960164 @default.
• W2003392551 cites W2062821569 @default.
• W2003392551 cites W2064047613 @default.
• W2003392551 cites W2068355326 @default.
• W2003392551 cites W2076794242 @default.
• W2003392551 cites W2094109632 @default.
• W2003392551 cites W2095003522 @default.
• W2003392551 cites W2097698114 @default.
• W2003392551 cites W2109689528 @default.
• W2003392551 cites W2124076816 @default.
• W2003392551 cites W2132268633 @default.
• W2003392551 cites W2134989772 @default.
• W2003392551 doi "https://doi.org/10.1111/cbdd.12402" @default.
• W2003392551 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/25092264" @default.
• W2003392551 hasPublicationYear "2014" @default.
• W2003392551 type Work @default.
• W2003392551 sameAs 2003392551 @default.
• W2003392551 citedByCount "3" @default.
• W2003392551 countsByYear W20033925512017 @default.
• W2003392551 crossrefType "journal-article" @default.
• W2003392551 hasAuthorship W2003392551A5003594028 @default.
• W2003392551 hasAuthorship W2003392551A5005009665 @default.
• W2003392551 hasAuthorship W2003392551A5036446709 @default.
• W2003392551 hasAuthorship W2003392551A5056074050 @default.
• W2003392551 hasAuthorship W2003392551A5078156446 @default.
• W2003392551 hasAuthorship W2003392551A5080076598 @default.
• W2003392551 hasConcept C11960822 @default.
• W2003392551 hasConcept C126661725 @default.
• W2003392551 hasConcept C143425029 @default.
• W2003392551 hasConcept C161790260 @default.
• W2003392551 hasConcept C170493617 @default.
• W2003392551 hasConcept C185592680 @default.
• W2003392551 hasConcept C193042331 @default.
• W2003392551 hasConcept C202751555 @default.
• W2003392551 hasConcept C2776568683 @default.
• W2003392551 hasConcept C2778866207 @default.
• W2003392551 hasConcept C2779438470 @default.
• W2003392551 hasConcept C42362537 @default.
• W2003392551 hasConcept C552990157 @default.
• W2003392551 hasConcept C55493867 @default.
• W2003392551 hasConcept C57992300 @default.
• W2003392551 hasConcept C64241487 @default.
• W2003392551 hasConcept C71240020 @default.
• W2003392551 hasConceptScore W2003392551C11960822 @default.
• W2003392551 hasConceptScore W2003392551C126661725 @default.
• W2003392551 hasConceptScore W2003392551C143425029 @default.
• W2003392551 hasConceptScore W2003392551C161790260 @default.
• W2003392551 hasConceptScore W2003392551C170493617 @default.
• W2003392551 hasConceptScore W2003392551C185592680 @default.
• W2003392551 hasConceptScore W2003392551C193042331 @default.
• W2003392551 hasConceptScore W2003392551C202751555 @default.
• W2003392551 hasConceptScore W2003392551C2776568683 @default.
• W2003392551 hasConceptScore W2003392551C2778866207 @default.
• W2003392551 hasConceptScore W2003392551C2779438470 @default.
• W2003392551 hasConceptScore W2003392551C42362537 @default.
• W2003392551 hasConceptScore W2003392551C552990157 @default.
• W2003392551 hasConceptScore W2003392551C55493867 @default.
• W2003392551 hasConceptScore W2003392551C57992300 @default.
• W2003392551 hasConceptScore W2003392551C64241487 @default.
• W2003392551 hasConceptScore W2003392551C71240020 @default.
• W2003392551 hasIssue "2" @default.
• W2003392551 hasLocation W20033925511 @default.
• W2003392551 hasLocation W20033925512 @default.
• W2003392551 hasOpenAccess W2003392551 @default.
• W2003392551 hasPrimaryLocation W20033925511 @default.
• W2003392551 hasRelatedWork W1975075764 @default.
• W2003392551 hasRelatedWork W1982680718 @default.
• W2003392551 hasRelatedWork W2003392551 @default.
• W2003392551 hasRelatedWork W2128093567 @default.
• W2003392551 hasRelatedWork W2178558875 @default.
• W2003392551 hasRelatedWork W2317458020 @default.
• W2003392551 hasRelatedWork W2517018940 @default.
• W2003392551 hasRelatedWork W2770541766 @default.
• W2003392551 hasRelatedWork W2793200717 @default.
• W2003392551 hasRelatedWork W2055165170 @default.

• next