【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。更多还原

【Abstract】 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.更多还原