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• W3178305855 endingPage "105160" @default.
• W3178305855 startingPage "105160" @default.
• W3178305855 abstract "Literature conclusively shows that one of the quinolinequinone analogs (6-anilino-5,8-quinolinequinone), referred to as LY83583 hereafter, an inhibitor of guanylyl cyclase, was used as the inhibitor of the cell proliferation in cancer cells. In the present work, a series of analogs of the LY83583 containing alkoxy group(s) in aminophenyl ring (AQQ1-15) were designed and synthesized via a two-step route and evaluated for their in vitro cytotoxic activity against four different cancer cell lines (K562, Jurkat, MT-2, and HeLa) and human peripheral blood mononuclear cells (PBMCs) by MTT assay. The analog (AQQ13) was identified to possess the most potent cytotoxic activity against K562 human chronic myelogenous (CML) cell line (IC50 = 0.59 ± 0.07 μM) with significant selectivity (SI = 4.51) compared to imatinib (IC50 = 5.46 ± 0.85 μM; SI = 4.60). Based on its superior cytotoxic activity, the analog AQQ13 was selected for further mechanistic studies including determination of its apoptotic effects on K562 cell line via annexin V/ethidium homodimer III staining potency, ABL1 kinase inhibitory activity, and DNA cleaving capacity. Results ascertained that the analog AQQ13 induced apoptosis in K562 cell line with notable DNA-cleaving activity. However, AQQ13 demonstrated weak ABL1 inhibition indicating the correlation between anti-K562 and anti-ABL1 activities. In continuance, respectively conducted in silico molecular docking and Absorption, Distribution, Metabolism, and Excretion (ADME) studies drew attention to enhanced binding interactions of AQQ13 towards DNA and its high compatibility with the potential limits of specified pharmacokinetic parameters making it as a potential anti-leukemic drug candidate. Our findings may provide a new insight for further development of novel quinolinequinone-based anticancer analogs against CML." @default.
• W3178305855 created "2021-07-19" @default.
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• W3178305855 date "2021-09-01" @default.
• W3178305855 modified "2023-10-01" @default.
• W3178305855 title "Design, synthesis and investigation of the mechanism of action underlying anti-leukemic effects of the quinolinequinones as LY83583 analogs" @default.
• W3178305855 cites W1747646526 @default.
• W3178305855 cites W1968120167 @default.
• W3178305855 cites W1971944126 @default.
• W3178305855 cites W1977043142 @default.
• W3178305855 cites W1981461449 @default.
• W3178305855 cites W1984361449 @default.
• W3178305855 cites W1987025912 @default.
• W3178305855 cites W1988500745 @default.
• W3178305855 cites W1997597792 @default.
• W3178305855 cites W2016138543 @default.
• W3178305855 cites W2017214640 @default.
• W3178305855 cites W2028267884 @default.
• W3178305855 cites W2032772141 @default.
• W3178305855 cites W2036291177 @default.
• W3178305855 cites W2043995349 @default.
• W3178305855 cites W2057442248 @default.
• W3178305855 cites W2065472817 @default.
• W3178305855 cites W2076038104 @default.
• W3178305855 cites W2084980511 @default.
• W3178305855 cites W2086945873 @default.
• W3178305855 cites W2088862428 @default.
• W3178305855 cites W2089325462 @default.
• W3178305855 cites W2094807012 @default.
• W3178305855 cites W2097498294 @default.
• W3178305855 cites W2104298012 @default.
• W3178305855 cites W2106602239 @default.
• W3178305855 cites W2123819766 @default.
• W3178305855 cites W2129706529 @default.
• W3178305855 cites W2135732933 @default.
• W3178305855 cites W2139783224 @default.
• W3178305855 cites W2145538332 @default.
• W3178305855 cites W2155739335 @default.
• W3178305855 cites W2168998560 @default.
• W3178305855 cites W2177617854 @default.
• W3178305855 cites W2180139391 @default.
• W3178305855 cites W2260437978 @default.
• W3178305855 cites W2304994032 @default.
• W3178305855 cites W2409717177 @default.
• W3178305855 cites W2509469063 @default.
• W3178305855 cites W2512350263 @default.
• W3178305855 cites W2519604159 @default.
• W3178305855 cites W2561010246 @default.
• W3178305855 cites W2569578041 @default.
• W3178305855 cites W2604514216 @default.
• W3178305855 cites W2746740747 @default.
• W3178305855 cites W2753850534 @default.
• W3178305855 cites W2762475172 @default.
• W3178305855 cites W2779140005 @default.
• W3178305855 cites W2791660712 @default.
• W3178305855 cites W2791907327 @default.
• W3178305855 cites W2810554058 @default.
• W3178305855 cites W2888277971 @default.
• W3178305855 cites W2904783872 @default.
• W3178305855 cites W2919506894 @default.
• W3178305855 cites W2947056101 @default.
• W3178305855 cites W2952005855 @default.
• W3178305855 cites W2952239856 @default.
• W3178305855 cites W2971360858 @default.
• W3178305855 cites W2972989232 @default.
• W3178305855 cites W2975784395 @default.
• W3178305855 cites W2979597925 @default.
• W3178305855 cites W2981664628 @default.
• W3178305855 cites W2985795334 @default.
• W3178305855 cites W2990286446 @default.
• W3178305855 cites W2996236479 @default.
• W3178305855 cites W3006514606 @default.
• W3178305855 cites W3029915622 @default.
• W3178305855 cites W3035404049 @default.
• W3178305855 cites W3046636224 @default.
• W3178305855 cites W3080617703 @default.
• W3178305855 cites W3093412469 @default.
• W3178305855 cites W3097159778 @default.
• W3178305855 cites W3147142721 @default.
• W3178305855 cites W572193077 @default.
• W3178305855 cites W2086725799 @default.
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• W3178305855 doi "https://doi.org/10.1016/j.bioorg.2021.105160" @default.
• W3178305855 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/34328861" @default.
• W3178305855 hasPublicationYear "2021" @default.
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