FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W4384156162> ?p ?o ?g. }

• W4384156162 abstract "Abstract In the current study, we designed and synthesized a series of new quinoline derivatives 10a-p as antiproliferative agents targeting cancer through inhibition of VEGFR-2. Preliminary molecular docking to assess the interactions of the designed derivatives with the binding site of VEGFR-2 (PDB code: 4ASD) displayed binding poses and interactions comparable to sorafenib. The synthesized compounds exhibited VEGFR-2 inhibitory activity with IC 50 ranging from 36 nM to 2.23 μM compared to sorafenib (IC 50 = 45 nM), where derivative 10i was the most potent. Additionally, the synthesized derivatives were evaluated in vitro for their cytotoxic activity against HepG2 cancer cell line. Seven compounds 10a , 10c , 10d , 10e , 10i , 10n and 10o (IC 50 = 4.60, 4.14, 1.07, 0.88, 1.60, 2.88 and 2.76 μM respectively) displayed better antiproliferative activity than sorafenib (IC 50 = 8.38 μM). Compound 10i was tested against Transformed Human Liver Epithelial-2 normal cell line (THLE-2) to evaluate its selective cytotoxicity. Furthermore, 10i , as a potent representative of the series, was assayed for its apoptotic activity and cell cycle kinetics’ influence on HepG2, its effects on the gene expression of VEGFR-2, and protein expression of the apoptotic markers Caspase-7 and Bax. Compound 10i proved to have a potential role in apoptosis by causing significant increase in the early and late apoptotic quartiles, a remarkable activity in elevating the relative protein expression of Bax and Caspase-7 and a significant reduction of VEGFR-2 gene expression. Collectively, the obtained results indicate that compound 10i has a promising potential as a lead compound for the development of new anticancer agents." @default.
• W4384156162 created "2023-07-14" @default.
• W4384156162 creator A5016721963 @default.
• W4384156162 creator A5021453491 @default.
• W4384156162 creator A5073430332 @default.
• W4384156162 creator A5078839649 @default.
• W4384156162 creator A5091150781 @default.
• W4384156162 date "2023-07-13" @default.
• W4384156162 modified "2023-09-27" @default.
• W4384156162 title "New proapoptotic chemotherapeutic agents based on the quinolone-3-carboxamide scaffold acting by VEGFR-2 inhibition" @default.
• W4384156162 cites W158280020 @default.
• W4384156162 cites W1967709626 @default.
• W4384156162 cites W1969368511 @default.
• W4384156162 cites W1970006188 @default.
• W4384156162 cites W1975654310 @default.
• W4384156162 cites W1985687906 @default.
• W4384156162 cites W1987364054 @default.
• W4384156162 cites W1995652272 @default.
• W4384156162 cites W2002014620 @default.
• W4384156162 cites W2020349068 @default.
• W4384156162 cites W2020391325 @default.
• W4384156162 cites W2038010347 @default.
• W4384156162 cites W2039112551 @default.
• W4384156162 cites W2063544208 @default.
• W4384156162 cites W2072945029 @default.
• W4384156162 cites W2083614629 @default.
• W4384156162 cites W2093258518 @default.
• W4384156162 cites W2096388250 @default.
• W4384156162 cites W2108384965 @default.
• W4384156162 cites W2113595687 @default.
• W4384156162 cites W2114570899 @default.
• W4384156162 cites W2114918609 @default.
• W4384156162 cites W2154502317 @default.
• W4384156162 cites W2177929699 @default.
• W4384156162 cites W2286433349 @default.
• W4384156162 cites W2315491646 @default.
• W4384156162 cites W2316405732 @default.
• W4384156162 cites W2318489807 @default.
• W4384156162 cites W2322050752 @default.
• W4384156162 cites W2333667010 @default.
• W4384156162 cites W2337121387 @default.
• W4384156162 cites W2344013879 @default.
• W4384156162 cites W2406309081 @default.
• W4384156162 cites W2553644649 @default.
• W4384156162 cites W2604219750 @default.
• W4384156162 cites W2626381435 @default.
• W4384156162 cites W2733738915 @default.
• W4384156162 cites W2768221484 @default.
• W4384156162 cites W2807489487 @default.
• W4384156162 cites W2896595935 @default.
• W4384156162 cites W2914410109 @default.
• W4384156162 cites W2916135772 @default.
• W4384156162 cites W2916750536 @default.
• W4384156162 cites W2934327251 @default.
• W4384156162 cites W2945036940 @default.
• W4384156162 cites W2952165053 @default.
• W4384156162 cites W2953945712 @default.
• W4384156162 cites W2959210265 @default.
• W4384156162 cites W2979183913 @default.
• W4384156162 cites W2981810096 @default.
• W4384156162 cites W2989644126 @default.
• W4384156162 cites W3037680403 @default.
• W4384156162 cites W3083233398 @default.
• W4384156162 cites W3087466970 @default.
• W4384156162 cites W3117503351 @default.
• W4384156162 cites W3127711546 @default.
• W4384156162 cites W3165720345 @default.
• W4384156162 cites W3170984450 @default.
• W4384156162 cites W3195417419 @default.
• W4384156162 cites W3196511077 @default.
• W4384156162 cites W4205689492 @default.
• W4384156162 cites W4206928090 @default.
• W4384156162 cites W4210774372 @default.
• W4384156162 cites W4284899546 @default.
• W4384156162 cites W4307210411 @default.
• W4384156162 cites W856882514 @default.
• W4384156162 doi "https://doi.org/10.1038/s41598-023-38264-w" @default.
• W4384156162 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/37443185" @default.
• W4384156162 hasPublicationYear "2023" @default.
• W4384156162 type Work @default.
• W4384156162 citedByCount "0" @default.
• W4384156162 crossrefType "journal-article" @default.
• W4384156162 hasAuthorship W4384156162A5016721963 @default.
• W4384156162 hasAuthorship W4384156162A5021453491 @default.
• W4384156162 hasAuthorship W4384156162A5073430332 @default.
• W4384156162 hasAuthorship W4384156162A5078839649 @default.
• W4384156162 hasAuthorship W4384156162A5091150781 @default.
• W4384156162 hasBestOaLocation W43841561621 @default.
• W4384156162 hasConcept C109316439 @default.
• W4384156162 hasConcept C12519072 @default.
• W4384156162 hasConcept C159110408 @default.
• W4384156162 hasConcept C185592680 @default.
• W4384156162 hasConcept C190283241 @default.
• W4384156162 hasConcept C202751555 @default.
• W4384156162 hasConcept C2778019345 @default.
• W4384156162 hasConcept C2778695046 @default.
• W4384156162 hasConcept C2779707156 @default.
• W4384156162 hasConcept C31573885 @default.
• W4384156162 hasConcept C41685203 @default.
• W4384156162 hasConcept C502942594 @default.

• next