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Synthesis and antimitotic activity of novel 5-aminoisoxazoles bearing alkoxyaryl moieties
被引:20
作者:
Vasilenko, Dmitry A.
[1
]
Averina, Elena B.
[1
,2
]
Zefirov, Nikolay A.
[1
]
Wobith, Birgit
[3
]
Grishin, Yuri K.
[1
]
Rybakov, Victor B.
[1
]
Zefirova, Olga N.
[1
,2
]
Kuznetsova, Tamara S.
[1
]
Kuznetsov, Sergei A.
[3
]
Zefirov, Nikolay S.
[1
,2
]
机构:
[1] Moscow MV Lomonosov State Univ, Dept Chem, Moscow 119991, Russia
[2] Russian Acad Sci, Inst Physiol Act Cpds, Chernogolovka 142432, Russia
[3] Univ Rostock, Inst Biol Sci Cell Biol & Biosyst Technol, D-18059 Rostock, Germany
基金:
俄罗斯基础研究基金会;
关键词:
ELECTROPHILIC ALKENES;
COMMON PHARMACOPHORE;
COLCHICINE SITE;
DRUG DESIGN;
ANALOGS;
HETEROCYCLIZATION;
TETRANITROMETHANE;
DERIVATIVES;
INHIBITORS;
ALCOHOLS;
D O I:
10.1016/j.mencom.2017.05.003
中图分类号:
O6 [化学];
学科分类号:
0703 ;
摘要:
5-Aminoisoxazoles containing trimethoxy- and methylenedioxyphenyl moieties were prepared by heterocyclization of electrophilic alkenes with tetranitromethane in the presence of triethylamine with subsequent reduction of resulting 5-nitroisoxazoles. The crystal structure of 3,4,5-trimethoxybenzyl 5-aminoisoxazole-3-carboxylate was determined by X-ray analysis. Two novel 5-aminoisoxazoles demonstrated moderate antimitotic activity to human lung carcinoma A549 cell line.
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收藏
页码:228 / 230
页数:3
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