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Matches in SemOpenAlex for { <https://semopenalex.org/work/W2045755433> ?p ?o ?g. }

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• W2045755433 abstract "Development of inhibitors of the drug efflux pump P-glycoprotein is a versatile approach to overcome multi drug resistance (MDR) in tumor therapy. In an approach to lower the conformational flexibility of the lead compound propafenone, we synthesized a set of dihydrobenzofuranes and benzopyranones. In the case of the 4 diastereomeric dihydrobenzofuranes, no significant differences in activity regarding the configuration on the side-chains at the dihydrofurane moiety (cis or trans) was observed. This may be due to the high flexibility of the side-chains, which still allow mutually overlap of pharmacophores. The benzopyranones showed a good correlation between lipophilicity and activity with gnerally lower log potency/log P ratios. This decrease may be due to the rigidization of the molecules. In an in silico screening approach, a set of diverse propafenone-type compounds was used to establish a pharmacophore model, which was used to screen the world drug index. Among the hits retrieved there are several compounds, which were previously described as MDR-modulators. This demonstrates the validity of the model." @default.
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• W2045755433 date "2003-03-01" @default.
• W2045755433 modified "2023-09-23" @default.
• W2045755433 title "In silico screening with benzofurane- and benzopyrane-type MDR-modulators" @default.
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• W2045755433 doi "https://doi.org/10.1016/s0014-827x(03)00021-1" @default.
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