Matches in SemOpenAlex for { <https://semopenalex.org/work/W3015297788> ?p ?o ?g. }
- W3015297788 endingPage "128177" @default.
- W3015297788 startingPage "128177" @default.
- W3015297788 abstract "Histone deacetylase enzymes are involved in the remodelling of chromatin and have a pivotal role in balancing acetylation and deacetylation status of chromatin eventually ensures the epigenetic regulation of gene expression. Its aberrant activity was reported in several forms of cancer considering it as a potential target for cancer treatment. Histone deacetylase inhibitors emerged as new class of antineoplastic drugs. Recent developments in understanding the mechanism of interaction between drug and targeted molecule encourages rational development of new class of HDAC inhibitors directing global or gene specific histone acetylation. In the present study, we designed 14 imidazole based derivatives abiding the common pharmacophore structure like CAP, Spacer, and Zinc binding group (ZBG) shared among the established HDAC inhibitors and was explored for its epigenetic modulator candidature targeting histone modifying enzymes through docking experiments. Among them the compound ethyl (2,5-diphenyl-1H-imidazole-4-yl)acetate (C3) was tightly bound to the isoforms of the HDAC enzymes at their receptor regions with high binding score. C3 was synthesized and have been characterized experimentally by IR and NMR techniques. The C3 inhibit cell proliferation of A549 lung cancer cell by inducing cytotoxicity and increased levels of ROS generation by disrupting mitochondrial permeability as evidenced from deflection in (Δψm). From this study we revealed that C3 a novel imidazole derivative inhibit highly expressed HDAC enzyme in non-small cell lung cancer cell lines by chromatin remodelling. Further findings may validate the identified compound C3 as an effective epigenetic modulator." @default.
- W3015297788 created "2020-04-17" @default.
- W3015297788 creator A5008788647 @default.
- W3015297788 creator A5012758029 @default.
- W3015297788 creator A5024873371 @default.
- W3015297788 creator A5033360475 @default.
- W3015297788 creator A5040485984 @default.
- W3015297788 creator A5061174068 @default.
- W3015297788 creator A5062580738 @default.
- W3015297788 creator A5091562248 @default.
- W3015297788 date "2020-08-01" @default.
- W3015297788 modified "2023-09-22" @default.
- W3015297788 title "Design and synthesis of imidazole based zinc binding groups as novel small molecule inhibitors targeting Histone deacetylase enzymes in lung cancer" @default.
- W3015297788 cites W1534396737 @default.
- W3015297788 cites W1709997767 @default.
- W3015297788 cites W1966514102 @default.
- W3015297788 cites W1985515161 @default.
- W3015297788 cites W1991966795 @default.
- W3015297788 cites W1996507777 @default.
- W3015297788 cites W2006781136 @default.
- W3015297788 cites W2007996284 @default.
- W3015297788 cites W2023473357 @default.
- W3015297788 cites W2051381895 @default.
- W3015297788 cites W2054881399 @default.
- W3015297788 cites W2117247812 @default.
- W3015297788 cites W2125298169 @default.
- W3015297788 cites W2167033556 @default.
- W3015297788 cites W2198369501 @default.
- W3015297788 cites W2222589778 @default.
- W3015297788 cites W2561958681 @default.
- W3015297788 cites W2892113269 @default.
- W3015297788 cites W4211075966 @default.
- W3015297788 cites W4255691026 @default.
- W3015297788 doi "https://doi.org/10.1016/j.molstruc.2020.128177" @default.
- W3015297788 hasPublicationYear "2020" @default.
- W3015297788 type Work @default.
- W3015297788 sameAs 3015297788 @default.
- W3015297788 citedByCount "11" @default.
- W3015297788 countsByYear W30152977882020 @default.
- W3015297788 countsByYear W30152977882021 @default.
- W3015297788 countsByYear W30152977882022 @default.
- W3015297788 countsByYear W30152977882023 @default.
- W3015297788 crossrefType "journal-article" @default.
- W3015297788 hasAuthorship W3015297788A5008788647 @default.
- W3015297788 hasAuthorship W3015297788A5012758029 @default.
- W3015297788 hasAuthorship W3015297788A5024873371 @default.
- W3015297788 hasAuthorship W3015297788A5033360475 @default.
- W3015297788 hasAuthorship W3015297788A5040485984 @default.
- W3015297788 hasAuthorship W3015297788A5061174068 @default.
- W3015297788 hasAuthorship W3015297788A5062580738 @default.
- W3015297788 hasAuthorship W3015297788A5091562248 @default.
- W3015297788 hasConcept C104317684 @default.
- W3015297788 hasConcept C119157956 @default.
- W3015297788 hasConcept C167227067 @default.
- W3015297788 hasConcept C185592680 @default.
- W3015297788 hasConcept C27253355 @default.
- W3015297788 hasConcept C2776262904 @default.
- W3015297788 hasConcept C2778305200 @default.
- W3015297788 hasConcept C41091548 @default.
- W3015297788 hasConcept C502942594 @default.
- W3015297788 hasConcept C55493867 @default.
- W3015297788 hasConcept C64927066 @default.
- W3015297788 hasConcept C71723506 @default.
- W3015297788 hasConcept C83640560 @default.
- W3015297788 hasConcept C86803240 @default.
- W3015297788 hasConceptScore W3015297788C104317684 @default.
- W3015297788 hasConceptScore W3015297788C119157956 @default.
- W3015297788 hasConceptScore W3015297788C167227067 @default.
- W3015297788 hasConceptScore W3015297788C185592680 @default.
- W3015297788 hasConceptScore W3015297788C27253355 @default.
- W3015297788 hasConceptScore W3015297788C2776262904 @default.
- W3015297788 hasConceptScore W3015297788C2778305200 @default.
- W3015297788 hasConceptScore W3015297788C41091548 @default.
- W3015297788 hasConceptScore W3015297788C502942594 @default.
- W3015297788 hasConceptScore W3015297788C55493867 @default.
- W3015297788 hasConceptScore W3015297788C64927066 @default.
- W3015297788 hasConceptScore W3015297788C71723506 @default.
- W3015297788 hasConceptScore W3015297788C83640560 @default.
- W3015297788 hasConceptScore W3015297788C86803240 @default.
- W3015297788 hasFunder F4320323670 @default.
- W3015297788 hasFunder F4320334771 @default.
- W3015297788 hasLocation W30152977881 @default.
- W3015297788 hasOpenAccess W3015297788 @default.
- W3015297788 hasPrimaryLocation W30152977881 @default.
- W3015297788 hasRelatedWork W1992075788 @default.
- W3015297788 hasRelatedWork W2052453190 @default.
- W3015297788 hasRelatedWork W2075984614 @default.
- W3015297788 hasRelatedWork W2094953745 @default.
- W3015297788 hasRelatedWork W2099440961 @default.
- W3015297788 hasRelatedWork W2155508219 @default.
- W3015297788 hasRelatedWork W2294019204 @default.
- W3015297788 hasRelatedWork W2552712024 @default.
- W3015297788 hasRelatedWork W4249777732 @default.
- W3015297788 hasRelatedWork W4289520319 @default.
- W3015297788 hasVolume "1214" @default.
- W3015297788 isParatext "false" @default.
- W3015297788 isRetracted "false" @default.
- W3015297788 magId "3015297788" @default.