中国药科大学学报2017，Vol.48Issue(4)：425-431,7.DOI:10.11665/j.issn.1000-5048.20170406
(噁)唑并[5,4-d]嘧啶类化合物的设计、合成及其抗肿瘤活性
Design, synthesis and antitumor activities of oxazolo[5, 4-d] pyrimidine derivatives
摘要
Abstract
A series of oxazole[5,4-d] pyrimidine derivatives were designed and synthesized to discover novel compounds with antitumor activity.Compounds 8a-8m were synthesized using acetamidine hydrochloride as the start material.The structures of synthesized compounds were confirmed by IR,1H NMR,EI-MS and elemental analysis.The antiangiogenesis activities of the synthesized compounds were determined by MTT in human umbilical vein endothelial cell (HUVEC).The in vitro antitumor activities of the synthesized compounds were determined by MTT assay in A549,HepG2 and U251.Compounds 8c,8d,8g,8i and 8l were found to inhibit the proliferation of all the tested cell lines.Compound 8l exhibited noteworthy activities in A549,HepG2 and U251 cell lines with IC50value lower than the positive reference sunitinib,suggesting that compound 8l might be the promising antitumor agent for further investigation.关键词
(噁)唑并[5,4-d]嘧啶类衍生物/合成/抗血管生成/抗肿瘤活性Key words
oxazole[5, 4-d] pyrimidine derivatives/synthesis/anti-angiogenesis/antitumor activity分类
医药卫生引用本文复制引用
李明涛,徐丹,薛文君,尤启冬,孙丽萍..(噁)唑并[5,4-d]嘧啶类化合物的设计、合成及其抗肿瘤活性[J].中国药科大学学报,2017,48(4):425-431,7.基金项目
国家自然科学基金资助项目(No.20872181,No.21172265)This study was supported by the National Natural Science Foundation of China (No.20872181,No.21172265) （No.20872181,No.21172265）
