Synthesis and Biological Evaluation of 4-Chlorocolchicine Derivatives as Potent Anticancer Agents with Broad Effective Dosage Ranges
Synthesis and Biological Evaluation of 4-Chlorocolchicine Derivatives as Potent Anticancer Agents with Broad Effective Dosage Ranges
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4-氯秋水仙碱衍生物作为有效剂量范围广泛的强效抗癌剂的合成和生物学评价
DOI：
10.1039/c2md20250f
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发表时间：
2012
期刊：
影响因子：
--
通讯作者：
and H. Takayama
中科院分区：
文献类型：
--
作者：
H. Nishiyama;M. Ono;T. Sugimoto;T.Sasai;N. Asakawa;T. Matsumoto;T. Yaegashi;M. Nagaoka;T. Matsuzaki;N. Kogure;M. Kitajima;and H. Takayama
从开发新型抗癌药物的角度出发，合成了4-氯秋水仙碱衍生物。研究了这些衍生物在小鼠体内的活性、有效剂量范围以及良好的代谢稳定性。结果表明，C-7氨基上含有α-羟基烷烃基的衍生物37和40具有较强的活性，有效剂量范围广。
4-Chlorocolchicine derivatives were synthesized with a view of developing new anticancer agents. The derivatives were examined for their potent activities and effective dosage ranges in mice, as well as favorable metabolic stabilities. As a result, derivatives 37 and 40, bearing an α-hydroxyalkanoyl group on the C-7 amino function, were revealed to exhibit potent activities with broad effective dosage ranges.