南方医科大学学报2011，Vol.31Issue(5)：875-877,3.
新结构嘧啶类化合物的合成及抗肿瘤活性筛选
Synthesis and antitumor activities of pyrimidines
摘要
Abstract
Objective To synthesize cyclin-dependent kinase (CDKs) inhibitors and assay their antitumor activities. Methods A series of pyrimidines containing different arylamino and l-(methylsulfonyl)piperidin moieties were designed by combining the segments l-(methylsulfonyl)piperidin and pyrimidine heterocycles according to the super-postion principle of the reinforcement of biological activities. Results Their structures were characterized by MS and 1H NMR spectra and all the synthesized compounds were screened for their antimicrobial activity with MTT assay. Conclusion The preliminary bioassay showed that compound 3b displayed good antitumor activity (IC50=13.6 μmol/L). The preliminary structure activity relationship analysis of these analogues suggest that the steric factor may have important impact on the anti-tumor activity.关键词
嘧啶/合成/抗肿瘤活性Key words
pyrimidines/synthesis/antitumor activities分类
医药卫生引用本文复制引用
游文玮,赵培亮,邹敏,周中振,段安娜,吴曙光..新结构嘧啶类化合物的合成及抗肿瘤活性筛选[J].南方医科大学学报,2011,31(5):875-877,3.基金项目
教育部博士点新教师基金(20104433120011) （20104433120011）
广东省自然科学基金(10451051501004725) （10451051501004725）
广东省医学科研基金(B2010185) （B2010185）
