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3'-C-甲基柔红霉素的合成及其抗肿瘤活性

Synthesis and antitumor activity of 3'-C-methyl-daunorubicin.

作者信息

Thang T T, Imbach J L, Fizames C, Lavelle F, Ponsinet G, Olesker A, Lukacs G

出版信息

Carbohydr Res. 1985 Jan 15;135(2):241-7. doi: 10.1016/s0008-6215(00)90775-4.

Abstract

Reaction of 1,5-anhydro-4-O-benzoyl-2,3,6-trideoxy-3-C-methyl-3-trifluoro-acetami no-L-lyxo-hex-1-enitol with daunomycinone in the presence of anhydrous toluene-p-sulfonic acid in benzene, followed by removal of the N- and O-protecting groups under mild conditions, gave 3'-C-methyldaunorubicin. The antitumor activity of the new anthracycline glycoside has been evaluated.

摘要

1,5-脱水-4-O-苯甲酰基-2,3,6-三脱氧-3-C-甲基-3-三氟乙酰氨基-L-来苏-己-1-烯醇与柔红霉素酮在苯中无水对甲苯磺酸存在下反应,然后在温和条件下去除N-和O-保护基,得到3'-C-甲基柔红霉素。已评估了这种新的蒽环类糖苷的抗肿瘤活性。

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Synthesis and antitumor activity of 3'-C-methyl-daunorubicin.3'-C-甲基柔红霉素的合成及其抗肿瘤活性
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3'-Hydroxyesorubicin. Synthesis and antitumor activity.3'-羟基表柔比星。合成与抗肿瘤活性。
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