目的 合成N-3，4，6，7-四氫-2H-取代嘧啶并[1，6-c]喹唑啉-2-烯胺類衍生物，并對其進行體外抗腫瘤活性研究。方法 以4，6-二氯嘧啶和6-氨基-1，4-苯并二氧雜環(huán)為起始原料，經(jīng)過氨化、Suzuki偶聯(lián)、縮合反應和環(huán)合反應合成一系列N-3，4，6，7-四氫-2H-取代嘧啶并[1，6-c]喹唑啉-2-烯胺類化合物，并采用MTT法對其體外腫瘤活性進行研究。結(jié)果 設(shè)計并合成了18個目標化合物，結(jié)構(gòu)經(jīng)¹H-NMR和MS確證。活性測試結(jié)果顯示多個目標化合物抗腫瘤活性與陽性對照藥索拉非尼相近。結(jié)論 發(fā)現(xiàn)了一類全新結(jié)構(gòu)的骨架分子，目標化合物具有較強的抗腫瘤活性，為新型抗腫瘤化合物的設(shè)計與合成提供思路。

Objective To synthesize N-3,4,6,7-tetrahydro-2H-pyrimido[1,6-c]quinazolin-2-imine derivatives, and to investigate their antitumor activities in vitro. Methods 2,6-Dichloropyrimidine and 6-amino-1,4-benzodioxole were used as starting materials to synthesize a series of 3,4,6,7-tetrahydro-2H-pyrimido[1,6-c]quinazolin-2-imine derivatives through amination, Suzuki couple reaction, condensation, and cyclization reaction. The antitumor activities in vitro were determined by MTT assay. Results Eighteen target compounds were designed and synthesized, and their chemical structures were confirmed by ¹H-NMR and MS. Antitumor activities test showed that some target compounds have as the same antitumor activities as sorafenib. Conclusion A novel skeleton molecular are discovered, and the targeted compounds have good antitumor activities, which offer new mentality to designe and synthesize novel antitumor compounds in the future.

福建省自然科學基金資助項目（2016J01352）；福建省省屬公益類科研院所基本科研專項（2015R1031-1）；福建省醫(yī)學科學研究院青年科研課題（201401）