FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4385623161> ?p ?o ?g. }

• W4385623161 endingPage "136358" @default.
• W4385623161 startingPage "136358" @default.
• W4385623161 abstract "The observed toxicity of newly designed anticancer drugs is considered as an impediment challenging phenomenon of intense concern arising from diversity in drug targets and the latter concern is therefore still in need for further research. The current investigation reports the design and synthesis of a new series of pyridine-thiazole hybrids and their derived 1,2,3-triazole analogues incorporating with varied sugar moieties and their acyclic analogues 3-11 and 13-18. The newly synthesized compounds were investigated for their cytotoxic activities against human liver HepG-2 and breast MCF-7 cancer cell lines. The pyridine-thiazolidinone-triazole based targets 16-18 revealed the potent cytotoxic activities. Also, all synthesized derivatives afforded promising safety antiproliferative margins against the normal human diploid cell line WI-38. The promising analogues 16-18 were further studied for their inhibitory assessment against EGFR and CDK-2/cyclin A2 kinases. The pyridine-thiazolidinone-1,2,3-triazole based glycosides 17 and 18 displayed promising and relatively equipotent inhibitory activity against EGFR enzyme compared with the reference drug, erlotinib (IC50= 0.19, 0.12, and 0.15 μM, respectively). While, the three glycosides 16-18 showed superior inhibitory potency against CDK-2/cyclin A2 kinases compared to the standard roscovitine (IC50 = 0.26, 0.22, 0.18 and 0.42 μM, respectively). The impact of triazole glycoside 18 upon cell cycle and apoptosis induction was determined to detect its mechanism of action. Additionally, it upregulated the levels of caspase-3, Bax and Bcl-2 in MCF-7 cells. Finally, molecular docking study was simulated to achieve a better rationalization and gain an insight into the binding affinity of the potent derivatives with their targeted enzymes, which prompts their application as optimum leads for further modification in the anticancer field." @default.
• W4385623161 created "2023-08-08" @default.
• W4385623161 creator A5061043109 @default.
• W4385623161 creator A5068325258 @default.
• W4385623161 creator A5069682913 @default.
• W4385623161 creator A5079748080 @default.
• W4385623161 creator A5080702730 @default.
• W4385623161 date "2023-12-01" @default.
• W4385623161 modified "2023-10-17" @default.
• W4385623161 title "Novel pyridine-thiazolidinone-triazole hybrid glycosides targeting EGFR and CDK-2: Design, synthesis, anticancer evaluation, and molecular docking simulation" @default.
• W4385623161 cites W1121361470 @default.
• W4385623161 cites W1974543775 @default.
• W4385623161 cites W1978615859 @default.
• W4385623161 cites W1983350693 @default.
• W4385623161 cites W1992361007 @default.
• W4385623161 cites W2004368209 @default.
• W4385623161 cites W2044214621 @default.
• W4385623161 cites W2082841583 @default.
• W4385623161 cites W2089655089 @default.
• W4385623161 cites W2114712929 @default.
• W4385623161 cites W2130921769 @default.
• W4385623161 cites W2143238584 @default.
• W4385623161 cites W2767814406 @default.
• W4385623161 cites W2793972506 @default.
• W4385623161 cites W2817198669 @default.
• W4385623161 cites W2907712775 @default.
• W4385623161 cites W2914376412 @default.
• W4385623161 cites W2921227021 @default.
• W4385623161 cites W2921954224 @default.
• W4385623161 cites W2979579230 @default.
• W4385623161 cites W2980047382 @default.
• W4385623161 cites W2981028192 @default.
• W4385623161 cites W3009121691 @default.
• W4385623161 cites W3022360542 @default.
• W4385623161 cites W3034999189 @default.
• W4385623161 cites W3042601174 @default.
• W4385623161 cites W3098535711 @default.
• W4385623161 cites W3115988672 @default.
• W4385623161 cites W3125885528 @default.
• W4385623161 cites W3159435427 @default.
• W4385623161 cites W3170695023 @default.
• W4385623161 cites W3183201628 @default.
• W4385623161 cites W3184782559 @default.
• W4385623161 cites W3189110082 @default.
• W4385623161 cites W3196777249 @default.
• W4385623161 cites W3215995278 @default.
• W4385623161 cites W4200492933 @default.
• W4385623161 cites W4213033615 @default.
• W4385623161 cites W4223550910 @default.
• W4385623161 cites W4282933028 @default.
• W4385623161 cites W4291788844 @default.
• W4385623161 cites W4295083870 @default.
• W4385623161 cites W4306673388 @default.
• W4385623161 cites W53566393 @default.
• W4385623161 doi "https://doi.org/10.1016/j.molstruc.2023.136358" @default.
• W4385623161 hasPublicationYear "2023" @default.
• W4385623161 type Work @default.
• W4385623161 citedByCount "0" @default.
• W4385623161 crossrefType "journal-article" @default.
• W4385623161 hasAuthorship W4385623161A5061043109 @default.
• W4385623161 hasAuthorship W4385623161A5068325258 @default.
• W4385623161 hasAuthorship W4385623161A5069682913 @default.
• W4385623161 hasAuthorship W4385623161A5079748080 @default.
• W4385623161 hasAuthorship W4385623161A5080702730 @default.
• W4385623161 hasConcept C124320809 @default.
• W4385623161 hasConcept C159110408 @default.
• W4385623161 hasConcept C170493617 @default.
• W4385623161 hasConcept C178790620 @default.
• W4385623161 hasConcept C184235292 @default.
• W4385623161 hasConcept C185592680 @default.
• W4385623161 hasConcept C190283241 @default.
• W4385623161 hasConcept C2777907353 @default.
• W4385623161 hasConcept C2778087573 @default.
• W4385623161 hasConcept C2779438470 @default.
• W4385623161 hasConcept C29537977 @default.
• W4385623161 hasConcept C41685203 @default.
• W4385623161 hasConcept C55493867 @default.
• W4385623161 hasConcept C71240020 @default.
• W4385623161 hasConcept C71924100 @default.
• W4385623161 hasConcept C98274493 @default.
• W4385623161 hasConceptScore W4385623161C124320809 @default.
• W4385623161 hasConceptScore W4385623161C159110408 @default.
• W4385623161 hasConceptScore W4385623161C170493617 @default.
• W4385623161 hasConceptScore W4385623161C178790620 @default.
• W4385623161 hasConceptScore W4385623161C184235292 @default.
• W4385623161 hasConceptScore W4385623161C185592680 @default.
• W4385623161 hasConceptScore W4385623161C190283241 @default.
• W4385623161 hasConceptScore W4385623161C2777907353 @default.
• W4385623161 hasConceptScore W4385623161C2778087573 @default.
• W4385623161 hasConceptScore W4385623161C2779438470 @default.
• W4385623161 hasConceptScore W4385623161C29537977 @default.
• W4385623161 hasConceptScore W4385623161C41685203 @default.
• W4385623161 hasConceptScore W4385623161C55493867 @default.
• W4385623161 hasConceptScore W4385623161C71240020 @default.
• W4385623161 hasConceptScore W4385623161C71924100 @default.
• W4385623161 hasConceptScore W4385623161C98274493 @default.
• W4385623161 hasFunder F4320310077 @default.
• W4385623161 hasLocation W43856231611 @default.

• next