期刊
STEROIDS
卷 77, 期 11, 页码 1075-1085出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.steroids.2012.05.003
关键词
Cycloaddition; Isoxazoles; Nitrile oxides; Cytotoxic activity
资金
- New Hungary Development Plan [TAMOP 4.2.1/B-09/1/KONV-2010-0005]
- Hungarian Scientific Research Fund [K 101659]
- European Union [TAMOP 4.2.1/B-09/1/KONV-2010-0005]
- European Regional Fund
Regioselective 1,3-dipolar cycloadditions of different aryl nitrile oxides to mestranol were carried out to furnish novel steroidal 17 alpha-isoxazoles in good to excellent yields. Copper(I) was found to be an efficient catalyst, accelerating the intermolecular ring-closures and leading exclusively to 3,5-disubstituted isoxazoles. The yields of the cycloadducts, however, were influenced by the substituents on the aromatic moiety of the 1,3-dipoles. Moreover, dehydration of the primary products resulted in the corresponding Delta(16.17) exo-heterocyclic derivatives. All the synthesized compounds were subjected to in vitro pharmacological studies of their antiproliferative effects relative to three human malignant cell lines (HeLa, MCF7 and A2780). (C) 2012 Elsevier Inc. All rights reserved.
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