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

Bosc JJ; Latxague L; Leger JM; Balzarini J; Forfar I; Jarry C; Guillon J

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

机译：新的β-D-阿拉伯糖呋喃（1'，2'：4,5）恶唑啉-和阿拉伯-嘧啶酮衍生物的合成及体外细胞抑制活性。

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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.

机译：通过D-（-）-阿拉伯糖的氨基恶唑啉的杂原子环化获得了一系列核苷衍生物。通过X射线结构分析获得了一些新的阿拉伯糖基嘧啶酮衍生物的立体结构的明确证据。然后评估这些新合成的化合物对鼠白血病（L1210）和人T淋巴细胞（Molt 4 / C8和CEM）的抑制细胞活性。在该系列的所有化合物中，受保护的甲硅烷基化的三环稠合嘧啶酮10对鼠白血病L1210（IC（50）= 6 microM）和人类T淋巴细胞Molt 4 / C8（IC（50））表现出最显着的抗肿瘤活性。 = 7.9 microM）和CEM / 0细胞系（IC（50）= 7.5 microM）。这些化合物均未显示出显着的抗病毒抑制活性。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第2期|共9页
作者
Bosc JJ; Latxague L; Leger JM; Balzarini J; Forfar I; Jarry C; Guillon J;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
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1. Synthesis and in vitro cytostatic activity of new beta-D-arabino furan(1',2':4,5)oxazolo- and arabino-pyrimidinone derivatives. [J] . Bosc JJ, Latxague L, Leger JM, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第2期

机译：新的β-D-阿拉伯糖呋喃（1'，2'：4,5）恶唑啉-和阿拉伯-嘧啶酮衍生物的合成及体外细胞抑制活性。
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Synthesis and in vitro cytostatic activity of new beta-D-arabino furan(1',2':4,5)oxazolo- and arabino-pyrimidinone derivatives.

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