摘要
通过成酯反应合成了一种新型喜树碱类衍生物,并将其命名为PCC0208021。PCC0208021对4种结直肠癌细胞株(LS180、HCT116、HT-29和CT-26)显示出良好的体外生长抑制活性,并能有效抑制2种结直肠癌细胞株(LS180和HCT116)的集落形成;它在体外酶学水平可抑制拓扑异构酶Ⅰ(Topo Ⅰ)的活性;分子对接研究表明PCC0208021与Topo Ⅰ具有较高的结合亲和力。新型喜树碱衍生物PCC0208021有望成为治疗结直肠癌的先导化合物。
A novel camptothecin derivative,designed PCC0208021 is synthesized via esterification reaction.PCC0208021 inhibits the proliferation in vitro against 4 colorectal cancer cell lines( LS180,HCT116,HT-29 and CT-26),and inhibits the colony formation in vitro against 2 colorectal cancer cell lines( LS180 and HCT116). Also,it can suppress the activity of Topo Ⅰ and display a high binding affinity in the molecular docking study,and thus is expected to become a lead compound for the treatment of colorectal cancer.
作者
李敏
魏颖杰
刘宗亮
邹方霞
王洪波
田京伟
LI Min;WEI Ying-jie;LIU Zong-liang;ZOU Fang-xia;WANG Hong-bo;TIAN Jing-wei(School of Pharmacy,Key Laboratory of Molecular Pharmacology and Drug Evaluation(Yantai University),Ministry of Education,Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong,Yantai University,Yantai 264005,China)
出处
《烟台大学学报（自然科学与工程版）》
CAS
2021年第4期436-441,共6页
Journal of Yantai University(Natural Science and Engineering Edition)
基金
国家自然科学基金资助项目NSFC(82073888)
山东省高等学校优秀青年创新团队资助项目(2019KJM009)。
