共 39 条
Synthesis and biological evaluation of diastereoisomerically pure N,O-nucleosides
被引:37
作者:
Bortolini, Olga
[1
]
De Nino, Antonio
[1
]
Eliseo, Tommaso
[2
]
Gavioli, Riccardo
[3
]
Maiuolo, Loredana
[1
]
Russo, Beatrice
[1
]
Sforza, Fabio
[3
]
机构:
[1] Univ Calabria, Dipartimento Chim, I-87036 Arcavacata Di Rende, CS, Italy
[2] Univ Roma Tor Vergata, Dipartimento Sci & Tecnol Chim, Rome, Italy
[3] Univ Ferrara, Dipartimento Biochim & Biol Mol, I-44100 Ferrara, Italy
关键词:
N;
O-Nucleosides;
1,3-Dipolar cycloaddition;
Cytotoxic activity;
1,3-DIPOLAR CYCLOADDITION REACTIONS;
INVERSE-ELECTRON DEMAND;
NUCLEOSIDE ANALOGS;
NITRONES;
DERIVATIVES;
ISOXAZOLIDINES;
1,3-CYCLOADDITION;
CONFIGURATION;
DFT;
D O I:
10.1016/j.bmc.2010.08.024
中图分类号:
Q5 [生物化学];
Q7 [分子生物学];
学科分类号:
071010 ;
081704 ;
摘要:
Several N,O-nucleosides have been synthesized in good yields by direct 1,3-dipolar cyclization methodology, in the absence of solvent. A remarkable cis stereoselectivity (de 98%) was observed by tuning the substituents on the nitrone moiety. A good number of these N, O-nucleosides have been evaluated for cytotoxic activity against selected cellular lines. Some of the tested compounds have proven to be potential antiproliferative drugs. (C) 2010 Elsevier Ltd. All rights reserved.
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页码:6970 / 6976
页数:7
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