Synthesis and cytotoxic activities of 1-benzylidine substituted beta-carboline derivatives.

Cao R; Yi W; Wu Q; Guan X; Feng M; Ma C; Chen Z; Song H; Peng W

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Synthesis and cytotoxic activities of 1-benzylidine substituted beta-carboline derivatives.

机译：1-苄基取代的β-咔啉衍生物的合成和细胞毒活性。

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A series of new beta-carboline derivatives, bearing a benzylidine substituent at position-1, has been prepared and evaluated in vitro against a panel of human cell lines. The N(2)-benzylated beta-carbolinium bromates represented the most interesting cytotoxic activities. In particular, compounds 19 were found to be the most potent compounds with IC(50) values lower than 5 microM against 10 strains human tumor cell lines. These results confirmed that the N(2)-benzyl substituent on the beta-carboline ring played an important role in the modulation of the cytotoxic activities and suggested that further development of such compounds may be interest.

机译：已经制备了一系列在位置1带有苄基取代基的新型β-咔啉衍生物，并在体外针对一组人类细胞系进行了评估。 N（2）-苄基化β-咔啉溴酸盐代表最有趣的细胞毒性活性。特别是，发现化合物19对10株人类肿瘤细胞株的IC（50）值低于5 microM的最有效化合物。这些结果证实，β-咔啉环上的N（2）-苄基取代基在细胞毒性活性的调节中起着重要作用，并暗示可能需要进一步开发此类化合物。

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《Bioorganic and Medicinal Chemistry Letters》 |2008年第24期|共4页
作者
Cao R; Yi W; Wu Q; Guan X; Feng M; Ma C; Chen Z; Song H; Peng W;
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正文语种 eng
中图分类药学;生物化学;
关键词
Beta-Carbolines; derivatives; Synthesis;

机译：β-咔啉;衍生物;合成;

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1. Synthesis and cytotoxic activities of 1-benzylidine substituted beta-carboline derivatives. [J] . Cao R, Yi W, Wu Q, Bioorganic and Medicinal Chemistry Letters . 2008,第24期

机译：1-苄基取代的β-咔啉衍生物的合成和细胞毒活性。
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Synthesis and cytotoxic activities of 1-benzylidine substituted beta-carboline derivatives.

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