54879-66-2Relevant academic research and scientific papers
Exploitation of a tuned oxidation with N -haloimides in the synthesis of caulibugulones A-D
Naciuk, Fabrício F.,Milan, Julio C.,Andre?o, Almir,Miranda, Paulo C.M.L.
, p. 5026 - 5030 (2013)
Marine alkaloids caulibugulones A-D were synthesized in six steps starting from the readily available 2,5-dimethoxybenzaldehyde. Pomeranz-Fritsch reaction of N-(2,5-dimethoxybenzyl)-N-(2,2-dimethoxyethyl)-2-nitrobenzenesulfonamide proceeded smoothly to gi
Synthesis of Indenoisoquinoliniums and Methods of Use
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Page/Page column 12, (2008/12/07)
Substituted indenoisoquinolinium compounds, and pharmaceutical formulations of substituted indenoisoquinolinium compounds are described. Also described are processes for preparing substituted indenoisoquinolinium compounds. Also described are methods for
Synthesis and mechanism of action studies of a series of norindenoisoquinoline topoisomerase I poisons reveal an inhibitor with a flipped orientation in the ternary DNA-enzyme-inhibitor complex as determined by X-ray crystallographic analysis
Ioanoviciu, Alexandra,Antony, Smitha,Pommier, Yves,Staker, Bart L.,Stewart, Lance,Cushman, Mark
, p. 4803 - 4814 (2007/10/03)
Several norindenoisoquinolines substituted with methoxy or methylenedioxy groups have been prepared and their anticancer properties evaluated in cancer cell cultures and in topoisomerase I inhibition assays. 2,3-Dimethoxy-8,9- methylenedioxy-11H-indeno[1,
α-Adrenergic Agents. 1. Direct-Acting α1 Agonists Related to Methoxamine
DeMarinis, R. M.,Bryan, W. M.,Shah, D. H.,Hieble, J. P.,Pendleton, R. G.
, p. 1432 - 1437 (2007/10/02)
A series of phenylethylamines related to methoxamine has been prepared and evaluated for direct α1-receptor agonist activity.It has been observed that for open-chain compounds such as methoxamine, in which the amine-containing portion is free to adopt numerous conformations, an hydroxyl group is necessary for direct α1-adrenergic activity.When the hydroxyl is removed, however, the direct component of activity is greatly reduced unless the amine is incorporated into a more sterically defined structure.From our studies we have concluded that in order for a phenylethylamine to be active as a direct α1-receptor agonist it should have a β nitrogen in a fully extended conformation relative to a substituted phenyl ring.For optimum potency, the nitrogen should be exocyclic to a saturated six-membered ring.It may be further incorporated exocyclic or endocyclic into an additional ring so long as the amine occupies a well-defined region of space relative to the aromatic portion of a molecule.The ED50 values of some of the more potent compounds as α1-receptor agonists are on the order of 1 * 10-7 M.
