【摘要】 癌症是困扰人类健康的重要疾病,治疗癌症的相关药物研究也一直是科学研究的热点之一.本研究中,我们设计合成一种基于亮氨酸氨基肽酶(LAP)的抗癌前药分子的中间体CPT-Leu-OH,该化合物以L-亮氨酸残基基团作为后续LAP特异性触发药物释放的识别基团,以喜树碱(CPT)作为抗癌药物分子,同时在该化合物的结构上保留有易于修饰的活性基团-羟基,有利于后续引入各种荧光信号输出基团,最终设计合成了一种基于亮氨酸氨基肽酶的前药分子,为LAP相关癌症的诊疗提供新的方法参考.更多还原

【Abstract】 Cancer poses an important threat to human health, and cancer-related researches have been the hot issues in scientific research for many years. In this paper, we designed and synthesized an intermediate(CPT-Leu-OH) for anticancer prodrug based on leucine aminopeptidase(LAP). The compound using L-leucine residue as the recognition moiety, camptothecin(CPT) as the anticancer drug, and CPT-Leu-OH also retains an active group hydroxyl which is convenient for introducing fluorophore as the fluorescent signal output groups, so as to construct the prodrugs based on leucine aminopeptidase, and finally provides a new method for LAP-related cancer diagnosis and treatment.更多还原