1260740-41-7Relevant academic research and scientific papers
Total Syntheses of the Amaryllidaceae Alkaloids Zephycandidine III and Lycosinine A and Their Evaluation as Inhibitors of Acetylcholinesterase
Xu, Xingjun,Kim, Hye-Sun,Chen, Wei-Min,Ma, Xiang,Correy, Galen J.,Banwell, Martin G.,Jackson, Colin J.,Willis, Anthony C.,Carr, Paul D.
, p. 4044 - 4053 (2017)
The title alkaloids, 1 and 2, have been prepared using cross-coupling chemistries and together with various analogues they have been evaluated for their capacity to inhibit acetylcholinesterase. Contrary to an earlier report, it was found that biaryl 1 is not a significant inhibitor of this enzyme, and neither are any of its congeners, including alkaloid 2.
Enantioselective, Catalytic Vicinal Difluorination of Alkenes
Scheidt, Felix,Sch?fer, Michael,Sarie, Jér?me C.,Daniliuc, Constantin G.,Molloy, John J.,Gilmour, Ryan
supporting information, p. 16431 - 16435 (2018/11/23)
The enantioselective, catalytic vicinal difluorination of alkenes is reported by II/IIII catalysis using a novel, C2-symmetric resorcinol derivative. Catalyst turnover via in situ generation of an ArIIIIF2 species is enabled by Selectfluor oxidation and addition of an inexpensive HF–amine complex. The HF:amine ratio employed in this process provides a handle for regioselective orthogonality as a function of Br?nsted acidity. Selectivity reversal from the 1,1-difluorination pathway (geminal) to the desired 1,2-difluorination (vicinal) is disclosed (>20:1 in both directions). Validation with electron deficient styrenes facilitates generation of chiral bioisosteres of the venerable CF3 unit that is pervasive in drug discovery (20 examples, up to 94:06 e.r.). An achiral variant of the reaction is also presented using p-TolI (up to >95 % yield).
BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF
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Paragraph 0557; 0591; 0777, (2017/02/28)
β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
CARBAZOLE COMPOUNDS AND METHODS OF USING SAME
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Paragraph 00136, (2015/02/25)
The present invention provides carbazole compounds of the formula (I), which can be used for treating microbial, protozoan, viral infections and cancer. ?
