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20(S)-7-烷(芳)酰基喜树碱的合成 被引量：1

Synthesis of 20 (S)-7-Alkyl (aryl)acyl-camptothecin
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摘要 20(S)-喜树碱(2)在过硫酸铵和硫酸亚铁作用下,以75%硫酸为溶剂,分别与戊醛和糠醛进行Minisci反应,制得20(S)-7-戊酰基喜树碱(1a)和20(S)-7-(2-糠酰基)喜树碱(1b),收率分别为81.3%和56.0%。对1a、1b和2用SRB法进行了人白血病(HL-60)、人胃癌细胞(BGC-823)、人肝癌细胞(Bel-7402)和人鼻咽癌细胞(KB)的体外抗肿瘤活性试验。结果显示,1a、1b对HL-60、BGC-823的抑制作用较2强;对Bel-7402和KB的抑制作用较2弱。 20（S）-7-Valeryl-camptothecin（1a） and 20（S）-7-（2-furoyl）-camptothecin（1b） were synthesized from 20（S）-camptothecin（2） and n-valeraldehyde or furaldehyde by Minisci reaction in the presence of（NH4）2S2O8 and FeSO4 in 75% sulfuric acid,respectively.The yields were 81.3% and 56.0%.The in vitro antitumor activities of compound 1a,1b and 2 were evaluated by Sulforhodamine B（SRB） assay against four human tumor cell lines,including HL-60,BCG-803,Bel-7402 and KB.The results showed that the inhibtion of compound 1a and 1b against HL-60 and BCG-803 was stronger than 2,but was weaker than 2 against Bel-7402 and KB.
作者 聂丽娟 路渊 李响敏 李群生
机构地区 南昌大学理学院化学系 南昌大学中德联合研究院 上海美迪西生物医药有限公司
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2010年第10期724-726,共3页 Chinese Journal of Pharmaceuticals
基金 科技部中小企业创新基金项目(06C26213600312) 江西省科技厅攻关项目(赣财教[2005]132)
关键词 20(S)-7-戊酰基喜树碱 20(S)-7-(2-糠酰基)喜树碱 抗肿瘤活性 合成 20（S）-7-valeryl-camptothecin 20（S）-7-（2-furoyl）-camptothecin antitumor activity synthesis
分类号 R979.1 [医药卫生—药品]
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参考文献14

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二级参考文献30

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中国医药工业杂志
2010年 第10期

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