论文部分内容阅读
目的：合成亲脂性叶酸拮抗剂２，４二氨基５甲基６取代苄胺基喹唑啉类化合物，并研究其对肿瘤细胞的抑制作用。方法：以邻甲苯胺为原料设计并合成喹唑啉类化合物；用四甲基偶氮唑蓝比色法和磺酰罗丹明Ｂ法测定其对肿瘤细胞的抑制作用。结果：该类化合物对Ｌ１２１０白血病细胞有较强的抑制作用。在已测定的部分化合物的药理结果中化合物Ｄ１、Ｄ３、Ｄ５和Ｄ６对人结肠癌ＨＣＴ８细胞，化合物Ｄ１～５对人红白血病Ｋ５６２细胞均有较强的抑制作用；化合物Ｄ１～６对人ＨＬ６０白血病细胞和人胃癌ＢＧＣ细胞均有一定的抑制作用。结论：该喹唑啉类化合物具有较强的抗肿瘤作用。
OBJECTIVE: To synthesize lipophilic antagonist 2,4-diamino-5-methyl-6-substituted benzylaminoquinazolines and study their inhibitory effects on tumor cells. Methods: The o-toluidine was used as the starting material to design and synthesize quinazoline compounds. The inhibitory effect on the tumor cells was determined by MTT method and sulfonyl rhodamine B method. Results: The compounds have a strong inhibitory effect on L1210 leukemia cells. Compounds D1, D3, D5 and D6 have been shown to have a strong inhibitory effect on human colon cancer HCT-8 cells and compounds D1-5 against human erythroleukemia K562 cells in the pharmacological results of some of the compounds already tested. Compounds D1 to 6 Human HL 60 leukemia cells and human gastric cancer BGC cells have some inhibitory effect. Conclusion: The quinazoline compounds have strong anti-tumor effect.