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首页> 外文期刊>Journal of Medicinal Chemistry >Synthesis and evaluation of several new (2-chloroethyl)nitrosocarbamates as potential anticancer agents.
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Synthesis and evaluation of several new (2-chloroethyl)nitrosocarbamates as potential anticancer agents.

机译：几种新的（2-氯乙基）亚硝基氨基甲酸酯类化合物的合成和评估作为潜在的抗癌药。

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摘要

Seven new (2-chloroethyl)nitrosocarbamates have been synthesized as potential anticancer alkylating agents. These compounds were designed with carrier moieties that would either act as prodrugs or confer water solubility. All compounds were screened in an in vitro panel of five human tumor cell lines: CAKI-1 (renal), DLD-1 (colon), NCI-H23 (lung), SK-MEL-28 (melanoma), and SNB-7 (CNS). Several agents showed good activity with IC(50) values in the range of 1-10 microg/mL against at least two of the cell lines. One compound, carbamic acid, (2-chloroethyl)nitroso-4-acetoxybenzyl ester (3), was selected for further study in vivo against intraperitoneally implanted P388 murine leukemia. In addition to the aforementioned compound, both carbamic acid, (2-chloroethyl)nitroso-4-nitrobenzyl ester (9) and carbamic acid, (2-chloroethyl)nitroso-2,3,4, 6-tetra-O-acetyl-1-alpha,beta-D-glucopyranose ester (24) were evaluated against subcutaneously implanted M5076 murine sarcoma in mice. None of these compounds were active in vivo.
机译：已经合成了七种新的（2-氯乙基）亚硝基氨基甲酸酯作为潜在的抗癌烷基化剂。这些化合物被设计成具有载体部分，该载体部分可以充当前药或赋予水溶性。所有化合物均在5种人类肿瘤细胞系的体外筛选中筛选：CAKI-1（肾脏），DLD-1（结肠），NCI-H23（肺），SK-MEL-28（黑色素瘤）和SNB-7 （CNS）。几种试剂对至少两种细胞系的IC（50）值在1-10 microg / mL范围内显示出良好的活性。选择一种化合物氨基甲酸，（2-氯乙基）亚硝基-4-乙酰氧基苄基酯（3），以进一步针对体内腹膜内植入的P388鼠白血病进行研究。除上述化合物外，氨基甲酸（2-氯乙基）亚硝基-4-硝基苄基酯（9）和氨基甲酸（2-氯乙基）亚硝基-2,3,4,6-四-O-乙酰基-对小鼠皮下植入的M5076鼠肉瘤评估了1-α，β-D-吡喃葡萄糖酯（24）。这些化合物在体内均无活性。

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