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新型取代硫嘧啶无环核苷及其硫代糖苷类似物的合成与体外抗肿瘤活性

Synthesis and in vitro antitumor activity of new substituted thiopyrimidine acyclic nucleosides and their thioglycoside analogs.

作者信息

El-Sayed Wael A, Rashad Aymn E, Awad Samir M, Ali Mamdouh M

机构信息

Photochemistry Department, National Research Center, El Dokki, Cairo, Egypt.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2009 Apr;28(4):261-74. doi: 10.1080/15257770902946165.

Abstract

Some new thiopyrimidine acyclic nucleosides and thioglycoside derivatives 3a-c, 4a-c, 6a,b, and 7a,b were synthesized. The cytotoxicity and antitumor evaluation of all prepared compounds have been tested in vitro against Ehrlich's ascites carcinoma cell line and their activity against glutathione peroxidase and catalase were reported. The role of the prepared compounds as free radical regulators and the therapeutic antitumor effect of a balanced generation of free radicals are discussed. Compounds 2, 3b, 3c, 4a, and 4c inhibited significantly in a dose dependent manner the growth of Ehrlich ascites carcinoma cells while the other compounds did not show any antitumor activity even at higher concentrations.

摘要

合成了一些新型硫代嘧啶无环核苷和硫代糖苷衍生物3a - c、4a - c、6a,b和7a,b。已对所有制备的化合物进行了体外细胞毒性和抗肿瘤评估,测试其对艾氏腹水癌细胞系的活性,并报告了它们对谷胱甘肽过氧化物酶和过氧化氢酶的活性。讨论了所制备化合物作为自由基调节剂的作用以及自由基平衡产生的治疗抗肿瘤效果。化合物2、3b、3c、4a和4c以剂量依赖性方式显著抑制艾氏腹水癌细胞的生长,而其他化合物即使在较高浓度下也未显示出任何抗肿瘤活性。

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