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- W2970178027 abstract "Stereo- and regioisomers of a series of N,N-bis(alkanol)amine aryl ester derivatives have been prepared and studied as multidrug resistance (MDR) modulators. The new compounds contain a 2-(methyl)propyl chain combined with a 3-, 5- or 7-methylenes long chain and carry different aromatic ester portions. Thus, these compounds have a methyl group on the 3-methylenes chain and represent branched homologues of previously studied derivatives. The introduction of the methyl group gives origin to a stereogenic center and consequently to (R) and (S) enantiomers. In the pirarubicin uptake assay on K562/DOX cell line these compounds showed good activity and efficacy and in many cases enantioselectivity was observed. Docking studies confirmed the influence of the stereocenter on the interaction in the P-gp pocket. The P-gp interaction mechanism and selectivity towards MRP1 and BCRP were also evaluated on MDCK transfected cells overexpressing the three transporters. Almost all these compounds inhibited both P-gp and BCRP, but only derivatives with specific structural characteristics showed MRP1 activity. Moreover, two compounds, (S)-3 and (R)-7, showed the ability to induce collateral sensitivity (CS) against MDR cells. Therefore, these two CS-promoting agents could be considered interesting leads for the development of selective cytotoxic agents for drug-resistant cells." @default.
- W2970178027 created "2019-09-05" @default.
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- W2970178027 date "2019-11-01" @default.
- W2970178027 modified "2023-10-18" @default.
- W2970178027 title "Design, synthesis and biological evaluation of stereo- and regioisomers of amino aryl esters as multidrug resistance (MDR) reversers" @default.
- W2970178027 cites W1857799540 @default.
- W2970178027 cites W1936299695 @default.
- W2970178027 cites W1965287659 @default.
- W2970178027 cites W1965455284 @default.
- W2970178027 cites W1970346993 @default.
- W2970178027 cites W1971866641 @default.
- W2970178027 cites W1976915106 @default.
- W2970178027 cites W1977594275 @default.
- W2970178027 cites W1980528153 @default.
- W2970178027 cites W1981140460 @default.
- W2970178027 cites W1981871034 @default.
- W2970178027 cites W1983974579 @default.
- W2970178027 cites W1986663325 @default.
- W2970178027 cites W1989064705 @default.
- W2970178027 cites W1999917099 @default.
- W2970178027 cites W2006434892 @default.
- W2970178027 cites W2008679330 @default.
- W2970178027 cites W2011495430 @default.
- W2970178027 cites W2016377328 @default.
- W2970178027 cites W2017323433 @default.
- W2970178027 cites W2019490712 @default.
- W2970178027 cites W2024306434 @default.
- W2970178027 cites W2024965589 @default.
- W2970178027 cites W2025253425 @default.
- W2970178027 cites W2025816743 @default.
- W2970178027 cites W2026398446 @default.
- W2970178027 cites W2028533496 @default.
- W2970178027 cites W2031407900 @default.
- W2970178027 cites W2034182297 @default.
- W2970178027 cites W2044053408 @default.
- W2970178027 cites W2045032952 @default.
- W2970178027 cites W2045362218 @default.
- W2970178027 cites W2052312932 @default.
- W2970178027 cites W2053848658 @default.
- W2970178027 cites W2062782200 @default.
- W2970178027 cites W2063837793 @default.
- W2970178027 cites W2065161846 @default.
- W2970178027 cites W2075747570 @default.
- W2970178027 cites W2080610464 @default.
- W2970178027 cites W2081213990 @default.
- W2970178027 cites W2081912151 @default.
- W2970178027 cites W2085010866 @default.
- W2970178027 cites W2102743211 @default.
- W2970178027 cites W2103891415 @default.
- W2970178027 cites W2108982217 @default.
- W2970178027 cites W2112001901 @default.
- W2970178027 cites W2119010359 @default.
- W2970178027 cites W2125074900 @default.
- W2970178027 cites W2133538529 @default.
- W2970178027 cites W2154548288 @default.
- W2970178027 cites W2162097287 @default.
- W2970178027 cites W2163186938 @default.
- W2970178027 cites W2164395620 @default.
- W2970178027 cites W2207885398 @default.
- W2970178027 cites W2234080940 @default.
- W2970178027 cites W2254041806 @default.
- W2970178027 cites W2341735629 @default.
- W2970178027 cites W2381727044 @default.
- W2970178027 cites W2414497324 @default.
- W2970178027 cites W2473090878 @default.
- W2970178027 cites W2553103457 @default.
- W2970178027 cites W2567161668 @default.
- W2970178027 cites W2578534622 @default.
- W2970178027 cites W2767184029 @default.
- W2970178027 cites W2767764775 @default.
- W2970178027 cites W2779730509 @default.
- W2970178027 cites W2784697242 @default.
- W2970178027 cites W2796185457 @default.
- W2970178027 cites W2926349815 @default.
- W2970178027 cites W4239139991 @default.
- W2970178027 cites W4242930200 @default.
- W2970178027 cites W4256442994 @default.
- W2970178027 cites W796154648 @default.
- W2970178027 doi "https://doi.org/10.1016/j.ejmech.2019.111655" @default.
- W2970178027 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/31494468" @default.
- W2970178027 hasPublicationYear "2019" @default.
- W2970178027 type Work @default.