An efficient synthesis of novel 3-（piperidin-4-yl）isoxazolo[4,5-d]pyrimidine scaffold has been designed and deveopled. A series of 5-phenylurea derivatives was synthesized using this method. Their cytotoxic activiti...An efficient synthesis of novel 3-（piperidin-4-yl）isoxazolo[4,5-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 IC50 s of 1.565 mmol/L and1.311 mmol/L, respectively. Furthermore, compound 20 and 21 also showed potent inhibitory activities against PI3 Kd with IC50 s of 0.286 mmol/L and 0.452 mmol/L, respectively. These results indicate that these 3-（piperidin-4-yl）isoxazolo[4,5-d]pyrimidine derivatives are novel antitumor agents through the inhibition of PI3 Kd.展开更多
基金supported by the National Natural Science Foundation of China (No. 81172914)Tang Aoqing Professorship research grant from Jilin UniversityChina and Changchun Discovery Sciences, Ltd.
文摘An efficient synthesis of novel 3-（piperidin-4-yl）isoxazolo[4,5-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 IC50 s of 1.565 mmol/L and1.311 mmol/L, respectively. Furthermore, compound 20 and 21 also showed potent inhibitory activities against PI3 Kd with IC50 s of 0.286 mmol/L and 0.452 mmol/L, respectively. These results indicate that these 3-（piperidin-4-yl）isoxazolo[4,5-d]pyrimidine derivatives are novel antitumor agents through the inhibition of PI3 Kd.
