54879-66-2Relevant articles and documents
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 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.