新型4-芳基-5,6,7,8-四氢喹唑啉-2-胺类化合物的合成及其生物活性研究

Synthesis and Biological Activities of Novel 4-Aryl-5,6,7,8-tetrahydroquinazolin-2-amine Derivatives

以α-蒎烯为原料,经加成-氧化后与多种芳香醛缩合制得中间体4-芳亚甲基异松蒎酮3a^3h,3a^3h与盐酸胍在叔丁醇钾催化作用下合成8种新型4-芳取代-5,6,7,8,-四氢喹唑啉-2-胺类化合物4a^4h.其结构经IR,1H NMR,13C NMR,GC-MS和元素分析表征.初步探讨了所合成化合物对人乳腺癌细胞MCF-7和人肺癌细胞A549的体外生物活性,结果显示部分化合物具有很好的抗肿瘤活性.

The intermediate compounds 4-arylidene isopinanones 3a^3h were synthesized by using α-pinene as starting material in three steps reaction including addition, oxidation, and condensation with aromatic aldehydes. Subsequently, eight new 4-aryl-5,6,7,8-tetrahydroquinazolin-2-amine derivatives 4a^4h were obtained by reacting 3a^3h with guanidine hydrochloride under t-BuOK. Their structures were characterized by IR, ^H NMR, ^13C NMR, GC-MS and elemental analysis. Biological activities of 4a^4h against MCF-7 （human breast cancer） and A549 （human lung cancer） were tested and the results showed that some of compounds exhibited good antitumor activity.