当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Synthesis and in vitro cytostatic activity of new beta-D-arabino furan[1',2':4,5]oxazolo- and arabino-pyrimidinone derivatives.

Synthesis and in vitro cytostatic activity of new beta-D-arabino furan[1',2':4,5]oxazolo- and arabino-pyrimidinone derivatives.

Abstract：

:A series of nucleoside derivatives was obtained via heteroatom annulation of the amino oxazoline of D-(-)-arabinose. Unequivocal proofs for the stereostructure of some new arabinosyl pyrimidinone derivatives were obtained by X-ray structure analysis. These newly synthesized compounds were then evaluated for their cytostatic activity against murine leukemia (L1210), and human T-lymphocytes (Molt 4/C8 and CEM). Of all the compounds in the series, the protected silylated tricyclic fused pyrimidinone 10 showed the most significant antitumor activity against murine leukemia L1210 (IC(50)=6 microM), and human T-lymphocytes cells Molt 4/C8 (IC(50)=7.9 microM) and CEM/0 cell lines (IC(50)=7.5 microM). None of the compounds exhibited significant antiviral inhibitory activities.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Bosc JJ,Latxague L,Léger JM,Balzarini J,Forfar I,Jarry C,Guillon J

doi

10.1016/j.ejmech.2009.10.032

subject

Has Abstract

pub_date

2010-02-01 00:00:00

pages

831-9

issue

2

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(09)00534-0

journal_volume

45

pub_type

杂志文章

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