7-去氮腺苷衍生物的合成及生物活性研究  

Studies on the synthesis of the derivatives of 7-deaza-adenosine and their biological activities

作　　者：张亮仁[1] 张云龙[1] 全漪[1] 张礼和[1] 

机构地区：[1]北京大学天然药物及仿生药物国家重点实验室,北京100083

出　　处：《中国药物化学杂志》2003年第2期63-66,共4页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金资助项目 (2 0 13 2 0 3 0 )

摘　　要：目的合成 7 位炔基修饰的 7 去氮腺苷衍生物 ,并对这些化合物的抗肿瘤活性及对细胞周期的影响进行考察。方法在Pd(PPh3) 4和CuI的催化下 ,5 碘 7 去氮腺苷与炔烃反应合成目标化合物 ,用MTT法评价化合物的抗肿瘤活性 ,用流氏细胞术考察化合物对细胞周期的影响。结果与结论合成了 4种 7 去氮腺苷衍生物 ,这些化合物对肿瘤细胞的生长具有中等强度的抑制活性 ,化合物 3a可使HL 60和KB细胞周期阻断在G1 期并使HL 60细胞产生凋亡 ,但对KB细胞不产生凋亡。Aim To synthesize alkynyl modified 7 deaza adenosine derivatives and investigate their antitumor activities.Methods The desired compounds were synthesized through the reaction of 7 deaza adenosine and alkyne under the catalysis of Pd(PPh 3) 4 and CuI,their activities were evaluated through the MTT assay method and cytometric analysis.Results and Conclusions Four kinds of alkynyl modified were synthesized.These synthetic compounds show strong inhibition activities to tumor cells′ proliferation.The cytometric analysis shows that compound 3a could block cell cycles of HL 60 and KB at the G 1 stage and induce HL 60 cell′s apoptosis.

关 键 词：药物化学 制备 化学合成 流氏细胞术 7-去氮腺苷 抗肿瘤 抗肿瘤活性 细胞周期 

分 类 号：R914[医药卫生—药物化学]