Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113336
Abstract: P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a phenomenon in which cells become resistant to structurally and mechanistically unrelated drugs resulting in low intracellular drug concentrations. It is one of the noteworthy problems in malignant tumor… read more here.
Keywords: mediated multidrug; reversal agents; mcf adr; glycoprotein mediated ... See more keywords
Discovery of potent inhibitors against P-glycoprotein-mediated multidrug resistance aided by late-stage functionalization of 2-(4-(pyridin-2-yl)phenoxy)pyridine analogue.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c00337
Abstract: SIS3 is a specific inhibitor of Smad3 that inhibits the TGFβ1-induced phosphorylation of Smad3. In this article, a variety of SIS3 derivatives were designed and synthesized to discover potential inhibitors against P-glycoprotein-mediated multidrug resistance to… read more here.
Keywords: mediated multidrug; late stage; inhibitors glycoprotein; aided late ... See more keywords
Different structures of berberine and five other protoberberine alkaloids that affect P-glycoprotein-mediated efflux capacity
Sign Up to like & getrecommendations! Published in 2018 at "Acta Pharmacologica Sinica"
DOI: 10.1038/s41401-018-0183-7
Abstract: Berberine, berberrubine, thalifendine, demethyleneberberine, jatrorrhizine, and columbamine are six natural protoberberine alkaloid (PA) compounds that display extensive pharmacological properties and share the same protoberberine molecular skeleton with only slight substitution differences. The oral delivery of… read more here.
Keywords: binding affinities; capacity; six compounds; glycoprotein mediated ... See more keywords
Loading docetaxel in β-cyclodextrin-based micelles for enhanced oral chemotherapy through inhibition of P-glycoprotein mediated efflux transport
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DOI: 10.1039/c7ra03180g
Abstract: Oral administration of BCS Class IV drugs still faces great challenges owing to their poor dissolubility in the gastro-intestinal (GI) tract and low permeation capacity across the GI membrane. Here, we constructed a β-cyclodextrin-based polymeric… read more here.
Keywords: glycoprotein mediated; dtx; inhibition glycoprotein; mediated efflux ... See more keywords
Overcoming P-Glycoprotein–Mediated Drug Resistance with Noscapine Derivatives
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DOI: 10.1124/dmd.118.083188
Abstract: The antitussive agent noscapine has been shown to inhibit the proliferation of cancer cells by disruption of tubulin dynamic. However, the efficacy of several anticancer drugs that inhibit tublin dynamics (vinca alkaloids and taxanes) is… read more here.
Keywords: overcoming glycoprotein; noscapine derivatives; glycoprotein mediated; drug ... See more keywords
Discovery of a Flavonoid FM04 as a Potent Inhibitor to Reverse P-Glycoprotein-Mediated Drug Resistance in Xenografts and Improve Oral Bioavailability of Paclitaxel
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms232315299
Abstract: Biotransformation of flavonoid dimer FD18 resulted in an active metabolite FM04. It was more druggable because of its improved physicochemical properties. FM04 (EC50 = 83 nM) was 1.8-fold more potent than FD18 in reversing P-glycoprotein… read more here.
Keywords: oral bioavailability; fd18; glycoprotein mediated; inhibitor ... See more keywords