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Synthesis and biological evaluation of 3-(piperidin-4-yl)isoxazolo[4,5-d]pyrimidine derivatives as novel PI3Kδ inhibitors
作者姓名:Jia-Lin Guo  Yun-Yong Liu  Ya-Zhong Pei
作者单位:1.The Center for Combinatorial Chemistry and Drug Discovery of Jilin University, School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China;2.Nanjing Gator MediTech Company, Ltd., Nanjing 211300, China
基金项目:This work was supported by the National Natural Science Foundation of China (No. 81172914) and Tang Aoqing Professorship research grant from Jilin University, China and Changchun Discovery Sciences, Ltd. The authors wish to thank Prof. Xu Bai for insightful discussions on chemical synthesis.
摘    要:


Synthesis and biological evaluation of 3-(piperidin-4-yl)isoxazolo[4,5-d]pyrimidine derivatives as novel PI3Kδ inhibitors
Jia-Lin Guo,Yun-Yong Liu,Ya-Zhong Pei.Synthesis and biological evaluation of 3-(piperidin-4-yl)isoxazolo[4,5-d]pyrimidine derivatives as novel PI3Kδ inhibitors[J].Chinese Chemical Letters,2015,26(10):1283-1288.
Authors:Jia-Lin Guo  Yun-Yong Liu  Ya-Zhong Pei
Institution:1.The Center for Combinatorial Chemistry and Drug Discovery of Jilin University, School of Pharmaceutical Sciences, Jilin University, Changchun 130021, China;2.Nanjing Gator MediTech Company, Ltd., Nanjing 211300, China
Abstract:An efficient synthesis of novel 3-(piperidin-4-yl)isoxazolo4, 5-d]pyrimidine scaffold has been designed and deveopled. A series of 5-phenylurea derivatives was synthesized using this method. Their cytotoxic activities against breast cancer cell line BT-474 were evaluated by CCK-8 assay. Most of them showed potent anti-proliferative activities, of which compound 20 and 21 exhibited IC50s of 1.565 μmol/L and 1.311 μmol/L, respectively. Furthermore, compound 20 and 21 also showed potent inhibitory activities against PI3Kδ with IC50s of 0.286 μmol/L and 0.452 μmol/L, respectively. These results indicate that these 3-(piperidin-4-yl)isoxazolo4, 5-d] pyrimidine derivatives are novel antitumor agents through the inhibition of PI3Kδ.
Keywords:Synthesis  Isoxazolopyrimidine  PI3Kδ inhibitors  Cytotoxicity  
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