- 3,4-Dihydroisoquinolinium Salt Derivatives
-
The present invention relates to 3,4-dihydroisoquinolinium salt derivatives. More specifically, the present invention relates to 3,4-dihydroisoquinolinium salt derivatives of the following chemical formula (I).
- -
-
Page/Page column 35
(2009/09/08)
-
- Potential cancer chemopreventive activity of simple isoquinolines, 1-benzylisoquinolines, and protoberberines
-
Seventeen simple isoquinolines, 15 1-benzylisoquinolines, and 19 protoberberines were tested for their inhibitory activities against Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol- 13-acetate (TPA) in Raji cells. Among the tested alkaloids, the inhibitory activity of all 1-benzylisoquinolines and 11 protoberberines was higher than that of β-carotene. The 1-benzylisoquinolines 19, 21, 22, 29, and 34 and protoberberines 41, 47-49, 51, 52, and 55 showed potent inhibitory effects on EBV-EA induction (96-100% inhibition at 1 × 103 mol ratio/TPA). These alkaloids were more active than the naturally occurring alkaloids, 23, 25, 33, 53, and 54. In addition, fifteen simple isoquinolines, eighteen 1-benzylisoquinolines and eight protoberberines were evaluated with respect to their ability to scavenge 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radicals. Nine simple isoquinolines, ten 1-benzylisoquinolines, and four protoberberines were more potent than α-tocopherol, and four 1-benzylisoquinolines, 20 and 28-30, exhibited potent activities (SC50 4.5-5.8 μM). Their activities were higher than the naturally occurring alkaloids, 23, 25, and 33. Therefore, some of the isoquinoline alkaloids indicating the high activity on both assays may be potentially valuable cancer chemopreventive agents. Structure-activity relationships are discussed for both tests.
- Cui, Wenhua,Iwasa, Kinuko,Tokuda, Harukuni,Kashihara, Akiko,Mitani, Yosuke,Hasegawa, Tomoko,Nishiyama, Yumi,Moriyasu, Masataka,Nishino, Hoyoku,Hanaoka, Miyoji,Mukai, Chisato,Takeda, Kazuyoshi
-
-
- Synthesis and radioligand binding studies of methoxylated 1,2,3,4-tetrahydroisoquinolinium derivatives as ligands of the apamin-sensitive Ca2+-activated K+ channels
-
Several methoxylated 1,2,3,4-tetrahydroisoquinoliniums derived from N-methyl-laudanosine and N-methyl-noscapine were synthesized and evaluated for their affinity for apamin-sensitive binding sites. The quaternary ammonium derivatives have a higher affinit
- Graulich, Amaury,Scuvée-Moreau, Jacqueline,Alleva, Livia,Lamy, Cédric,Waroux, Olivier,Seutin, Vincent,Liégeois, Jean-Fran?ois
-
p. 7208 - 7214
(2007/10/03)
-
- 3,4-DIHYDROISOQUINOLINIUM SALT DERIVATIVES
-
The present invention relates to 3,4-dihydroisoquinolinium salt derivatives. More specifically, the present invention relates to 3,4-dihydroisoquinolinium salt derivatives of the following chemical formula (I).
- -
-
Page/Page column 74-75
(2008/06/13)
-
- Synthesis of a small library of phenylalkylamide derivatives as melatoninergic ligands for human mt1 and MT2 receptors
-
Focused small libraries of melatonin receptor ligands from arylalkylamine derivatives were synthesised by combinatorial chemistry using the mix and split method in the solid phase. A library of 108 compounds was then synthesised from 12 arylalkyl amines and nine carboxylic acids. The compound mixtures were evaluated on chicken brain melatonin and recombinant human mt1 and MT2 receptors. Deconvolution of the most potent mixture demonstrated the superiority of 3-methoxy and 2,5-dimethoxy substitution on the phenyl ring with isopropyl, propyl and ethyl amido chains. Several compounds with nanomolar affinity for human melatonin receptors were obtained. (C) 2000 Elsevier Science Ltd.
- Pegurier, C.Ecile,Curtet, Sophie,Nicolas, Jean-Paul,Boutin, Jean A.,Delagrange, Philippe,Renard, Pierre,Langlois, Michel
-
p. 163 - 171
(2007/10/03)
-
- Mapping the Melatonin Receptor. 4. Comparison of the Binding Affinities of a Series of Substituted Phenylalkyl Amides
-
A series of 2-, 3-, and 4-substituted phenylalkyl amides were prepared as potential melatonin analogs in order to investigate the nature of the binding site of the melatonin receptor in chicken brain.The length of the alkyl chain was systematically varied
- Garratt, Peter J.,Travard, Sylvie,Vonhoff, Stefan,Tsotinis, Andrew,Sugden, David
-
p. 1796 - 1805
(2007/10/03)
-