Synthesis and cytotoxic evaluation of C-9 oxidized podophyllotoxin derivatives.

CastroMA; Miguel-del-CorralJM; GordalizaM; GarciaPA; Gomez-ZuritaMA; San-FelicianoA

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Synthesis and cytotoxic evaluation of C-9 oxidized podophyllotoxin derivatives.

机译：C-9氧化鬼臼毒素衍生物的合成和细胞毒性评估。

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摘要

A series of podophyllotoxin and podophyllic aldehyde derivatives, lacking the lactone ring and oxidized at C-9 position, has been prepared. The functionalities considered at C-9 were carboxylic acids and several derivatives such as esters, amides, nitriles or anhydrides. The synthesized compounds were cytotoxic at the micromolar level, though less potent and selective than the parent compounds, revealing the influence of the C-9 electrophilic character on the potency and selectivity of these cyclolignans.

机译：已经制备了一系列缺乏内酯环并且在C-9位置被氧化的鬼臼毒素和鬼臼醛衍生物。 C-9处考虑的官能团是羧酸和几种衍生物，例如酯，酰胺，腈或酸酐。合成的化合物在微摩尔水平上具有细胞毒性，尽管其效力和选择性均低于母体化合物，从而揭示了C-9亲电特性对这些环木脂素的效力和选择性的影响。

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来源
《Bioorganic and Medicinal Chemistry》 |2007年第4期|P.1670-1678|共9页
作者
CastroMA; Miguel-del-CorralJM; GordalizaM; GarciaPA; Gomez-ZuritaMA; San-FelicianoA;
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作者单位

Departamento de Quimica Farmaceutica, Facultad de Farmacia, Campus Miguel de Unamuno, Universidad de Salamanca, 37007 Salamanca, Spain. macg@usal.es;

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原文格式 PDF
正文语种 eng
中图分类药学;生物化学;
关键词
Carbon ion; derivatives; Synthesis; Evaluation;

机译：碳离子衍生物合成评价;

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1. Synthesis and cytotoxic evaluation of C-9 oxidized podophyllotoxin derivatives. [J] . Castro MA, Miguel-del-Corral JM, Gordaliza M, Bioorganic and medicinal chemistry . 2007,第4期

机译：C-9氧化鬼臼毒素衍生物的合成和细胞毒性评估。
2. Synthesis and cytotoxic evaluation of C-9 oxidized podophyllotoxin derivatives [J] . M Angeles Castro, Jose M. Miguel del Corral, Marina Gordaliza, Bioorganic and Medicinal Chemistry . 2007,第4期

机译：C-9氧化鬼臼毒素衍生物的合成及细胞毒性评价
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Synthesis and cytotoxic evaluation of C-9 oxidized podophyllotoxin derivatives.

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