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- W3092022963 endingPage "104364" @default.
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- W3092022963 abstract "In this work, the synthesis of interesting urea derivatives 5 based on 1,4-dihydropyridines 3 is described for the first time. Considering that both families exhibit potential as drugs to treat various diseases, their activity as anticancer agents has been evaluated in HeLa (cervix), Jurkat (leukaemia) and A549 (lung) cancer cell lines as well as on healthy mice in vivo. In general, whereas 1,4-dihydropyridines show a moderate cytotoxic activity, their urea analogues cause an extraordinary increase in their antiproliferative activity, specially towards HeLa cells. Because of the chiral nature of these compounds, enantiomerically enriched samples were also tested, showing different cytotoxic activity than the racemic mixture. Although the reason is not clear, it could be caused by a complex amalgam of physical and chemical contributions. The studied compounds also exhibit luminescent properties, which allow performing a biodistribution study in cancer cells. They have emission maxima between 420 and 471 nm, being the urea derivatives in general red shifted. Emission quenching was observed for those compounds containing a nitro group (3e,f and 5e,f). Fluorescence microscopy showed that 1,4-dihydropyridines 3a and 3g localised in the lysosomes, in contrast to the urea derivatives 5h that accumulated in the cell membrane. This different distribution could be key to explain the differences found in the cytotoxic activity and in the mechanism of action. Interestingly, a preliminary in vivo study regarding the acute toxicity of some of these compounds on healthy mice has been conducted, using a concentration up to 7200 times higher than the corresponding IC50 value. No downgrade in the welfare of the tested mice was observed, which could support their use in preclinical tumour models." @default.
- W3092022963 created "2020-10-15" @default.
- W3092022963 creator A5008235537 @default.
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- W3092022963 date "2020-12-01" @default.
- W3092022963 modified "2023-10-15" @default.
- W3092022963 title "Novel ureido-dihydropyridine scaffolds as theranostic agents" @default.
- W3092022963 cites W1503588437 @default.
- W3092022963 cites W1540036423 @default.
- W3092022963 cites W1670095596 @default.
- W3092022963 cites W1964666522 @default.
- W3092022963 cites W1967920937 @default.
- W3092022963 cites W1973492721 @default.
- W3092022963 cites W1973678338 @default.
- W3092022963 cites W1974545418 @default.
- W3092022963 cites W1978971065 @default.
- W3092022963 cites W1980411311 @default.
- W3092022963 cites W1983321351 @default.
- W3092022963 cites W1984883623 @default.
- W3092022963 cites W1985578628 @default.
- W3092022963 cites W1986406178 @default.
- W3092022963 cites W1990568610 @default.
- W3092022963 cites W1991053537 @default.
- W3092022963 cites W1992118247 @default.
- W3092022963 cites W1992985769 @default.
- W3092022963 cites W1996822064 @default.
- W3092022963 cites W1997077390 @default.
- W3092022963 cites W1997605246 @default.
- W3092022963 cites W1998171707 @default.
- W3092022963 cites W1999871321 @default.
- W3092022963 cites W2002123777 @default.
- W3092022963 cites W2008772310 @default.
- W3092022963 cites W2008841091 @default.
- W3092022963 cites W2024203270 @default.
- W3092022963 cites W2025620439 @default.
- W3092022963 cites W2025740579 @default.
- W3092022963 cites W2027935944 @default.
- W3092022963 cites W2043974985 @default.
- W3092022963 cites W2048369407 @default.
- W3092022963 cites W2048438268 @default.
- W3092022963 cites W2064707725 @default.
- W3092022963 cites W2065471096 @default.
- W3092022963 cites W2066694476 @default.
- W3092022963 cites W2071634601 @default.
- W3092022963 cites W2072916054 @default.
- W3092022963 cites W2073397405 @default.
- W3092022963 cites W2082841583 @default.
- W3092022963 cites W2088540319 @default.
- W3092022963 cites W2090479207 @default.
- W3092022963 cites W2091549874 @default.
- W3092022963 cites W2092764012 @default.
- W3092022963 cites W2105462087 @default.
- W3092022963 cites W2106132819 @default.
- W3092022963 cites W2110778299 @default.
- W3092022963 cites W2112949474 @default.
- W3092022963 cites W2114611012 @default.
- W3092022963 cites W2120829433 @default.
- W3092022963 cites W2123280263 @default.
- W3092022963 cites W2124662474 @default.
- W3092022963 cites W2126559170 @default.
- W3092022963 cites W2127182686 @default.
- W3092022963 cites W2127980322 @default.
- W3092022963 cites W2130408125 @default.
- W3092022963 cites W2138497443 @default.
- W3092022963 cites W2140802449 @default.
- W3092022963 cites W2143395453 @default.
- W3092022963 cites W2147132125 @default.
- W3092022963 cites W2148160969 @default.
- W3092022963 cites W2149531351 @default.
- W3092022963 cites W2154908503 @default.
- W3092022963 cites W2158604280 @default.
- W3092022963 cites W2163008413 @default.
- W3092022963 cites W2167609389 @default.
- W3092022963 cites W2172216246 @default.
- W3092022963 cites W2181695372 @default.
- W3092022963 cites W2190579295 @default.
- W3092022963 cites W2203921412 @default.
- W3092022963 cites W2253963543 @default.
- W3092022963 cites W2280268793 @default.
- W3092022963 cites W2280540393 @default.
- W3092022963 cites W2293439596 @default.
- W3092022963 cites W2295852652 @default.
- W3092022963 cites W2321911469 @default.
- W3092022963 cites W2335179795 @default.
- W3092022963 cites W2341769195 @default.
- W3092022963 cites W2350104138 @default.
- W3092022963 cites W2478427153 @default.
- W3092022963 cites W2484149184 @default.
- W3092022963 cites W2485777383 @default.
- W3092022963 cites W2513899066 @default.
- W3092022963 cites W2572325958 @default.
- W3092022963 cites W2601148710 @default.
- W3092022963 cites W2608606389 @default.