- An enzyme-responsive and photoactivatable carbon-monoxide releasing molecule for bacterial infection theranostics
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Infections caused by pathogenic bacteria, especially the drug-resistant bacteria, are posing a devastating threat to public health, which underscores the urgent needs for advanced strategies to effectively prevent and treat these intractable issues. Here
- Wang, Xianghong,Chen, Xin,Song, Lingjie,Zhou, Rongtao,Luan, Shifang
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p. 9325 - 9334
(2020/11/03)
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- Compound as well as preparation method and application thereof
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The invention provides a compound as well as a preparation method and application thereof. The compound with the structure as shown in the formula (I) provided by the invention can be detected in realtime through a fluorescence technology by selecting a s
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Paragraph 0080-0083
(2020/01/08)
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- Synthesis and biological evaluation of flavones and benzoflavones as inhibitors of BCRP/ABCG2
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Multidrug resistance (MDR) often leads to a failure of cancer chemotherapy. Breast Cancer Resistance Protein (BCRP/ABCG2), a member of the superfamily of ATP binding cassette proteins has been found to confer MDR in cancer cells by transporting molecules with amphiphilic character out of the cells using energy from ATP hydrolysis. Inhibiting BCRP can be a solution to overcome MDR.We synthesized a series of flavones, 7,8-benzofl avones and 5,6-benzo flavones with varying substituents at positions 3, 3′ and 4′ of the (benzo)fl avone structure. All synthesized compounds were tested for BCRP inhibition in Hoechst 33342 and pheophorbide A accumulation assays using MDCK cells expressing BCRP. All the compounds were further screened for their P-glycoprotein (P-gp) and Multidrug resistance-associated protein 1 (MRP1) inhibitory activity by calcein AM accumulation assay to check the selectivity towards BCRP. In addition most active compounds were investigated for their cytotoxicity. It was observed that in most cases 7,8-benzoflavones are more potent in comparison to the 5,6-benzoflavones. In general it was found that presence of a 3-OCH3 substituent leads to increase in activity in comparison to presence of OH or no substitution at position 3. Also, it was found that presence of 3′,4′-OCH3 on phenyl ring lead to increase in activity as compared to other substituents. Compound 24, a 7,8-benzoflavone derivative was found to be most potent being 50 times selective for BCRP and showing very low cytotoxicity at higher concentrations.
- Juvale, Kapil,Stefan, Katja,Wiese, Michael
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p. 115 - 126
(2013/10/01)
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- Use of Hypervalent Iodine Oxidation for the C(3)-Hydroxylation of Chromone, Flavone and α-Naphthoflavone
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C(3)-Hydroxylation of chromone (1a), flavone (1b) and α-naphthoflavone (4) via acid-catalysed hydrolysis of the corresponding β-methoxy-α-hydroxydimethylacetals (2a, 2b, and 5) formed by iodobenzene diacetate-potassium hydroxide methanol oxidation is described.
- Moriarty, Robert M.,Prakash, Om,Musallam, H. A.
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p. 583 - 584
(2007/10/02)
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