- Peganumine A alkaloid structure simplifier and application thereof
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The invention discloses a Peganumine A alkaloid structure simplifier, a stereoisomer or a pharmaceutical salt thereof. The structure is shown in the following general formula: each substituent group is defined in the specification. The simplified structure of the Peganumine A alkaloid provided by the invention has a relatively obvious proliferation inhibition effect on liver cancer HepG2, lung cancer A549 and intestinal cancer HCT116, and the anti-tumor activity of part of compounds is higher than the anti-liver cancer HepG2 activity of Peganumine A reported in literatures.
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Paragraph 0037-0038; 0042-0044; 0064-0066
(2021/06/26)
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- 3-(Phenethylamino)demethyl(oxy)aaptamine as an anti-dormant mycobacterial substance: Isolation, evaluation and total synthesis
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3-(Phenethylamino)demethyl(oxy)aaptamine (1) was re-discovered from the marine sponge of Aaptos sp. as an anti-dormant mycobacterial substance through the bioassay-guided separation. Compound 1 showed potent anti-microbial activity against Mycobacterium bovis BCG with a minimum inhibitory concentration of 0.75 μg/mL under both aerobic conditions and hypoxic conditions inducing dormant state. Compound 1 was also effective against pathogenic M. tuberculosis strains including clinical multidrug-resistant strains. Furthermore, the successful total syntheses of 1 and its analog 3-aminodemethyl(oxy)aaptamine (2) afford sufficient quantities for further biological studies.
- Arai, Masayoshi,Han, Chisu,Jacobs, William R.,Kamiya, Kentaro,Kotoku, Naoyuki,Setiawan, Andi,Sumii, Yuji,Vilchèze, Catherine
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- PHARMACEUTICAL COMPOUNDS
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This application describes substituted 1,3,4,6,7,11b-hexahydro-benzo(a)quinolizine compounds, pharmaceutical compositions containing them, processes for making them and their therapeutic methods.
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Page/Page column 34-35
(2010/04/30)
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- Synthesis of the Marine Alkaloids Aaptamine and Demethyloxyaaptamine and of the Parent Structure Didemethoxyaaptamine
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The first synthesis of the novel marine alkaloids aaptamine and demethyloxyaaptamine is described, as well as the first synthesis of the parent heterocycle 1H-benzonaphthyridine (didemethoxyaaptamine).
- Pelletier, Jeffrey C.,Cava, Michael P.
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p. 616 - 622
(2007/10/02)
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