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目的:新型氮杂多肽酰肼类衍生物的设计和合成及其抗肿瘤活性研究。方法:以脯氨酸甲酯盐酸盐为原料,通过与苄氧羰基丙氨酸反应,在肼中肼解,得到所需中间体,进而与富马酸单酯反应得到目标化合物;和溴乙酸叔丁酯反应,三氟乙酸中脱去叔丁氧基,再与取代胺或氨水反应得到目标化合物。用MTT法测试合成的氮杂多肽酰肼类衍生物对肿瘤细胞的抑制活性。结果:合成了10个氮杂多肽酰肼类衍生物,其中有6个化合物对肿瘤细胞表现出抑制活性。结论:初步建立了氮杂多肽酰肼类衍生物的合成方法及其对肿瘤细胞抑制活性的构效关系。
AIM: To study the design and synthesis of novel aza - polypeptide hydrazide derivatives and their anti - tumor activity. Methods: The proline methyl ester hydrochloride was used as the starting material to obtain the desired intermediate by reaction with benzyloxycarbonylalanine in hydrazine to obtain the desired intermediate, which was further reacted with fumaric acid monoester to obtain the target compound. Bromine Tert-butyl acetate, trifluoroacetic acid removed tert-butoxy, and then with the amine or ammonia to react to give the target compound. The inhibitory activity of the synthesized aza-polypeptide hydrazide derivatives on tumor cells was tested by MTT assay. Results: Ten aza-peptide hydrazide derivatives were synthesized. Among them, six compounds showed inhibitory activity on tumor cells. CONCLUSION: The synthetic method of aza-hydrazide derivatives and their structure-activity relationship with tumor cell inhibitory activity were preliminarily established.