Currently, controllable linker cleavage at the target site will facilitate the clinical treatment of cancer. Dual-functional prodrugs in combination of carbohydrate as targeting group and pH-sensitive cleavable linker are desired in clinical development. Here, a qualified structure of N-phenylcarbamate-d-gluconhydroximo-1,5-lactam was employed and proved to be a potential candidate prodrug in the drug design. To proof this concept, the possible mechanism of Beckmann rearrangement and the degraded products were confirmed by HPLC and LC-MS under the acid condition mimic lysosome. Hence, the strategy of d-gluconhydroximo-1,5-lactam as a prodrug carrier fabricated with interested drugs will provide a great potential approach for chemotherapy.

中文翻译：

---

通过LC-MS表征pH敏感的可裂解D-gluconhydroximo-1，5-内酰胺水解物的化学特征：一种促进肿瘤靶向药物递送的潜在药物。

当前，在靶位点的可控接头裂解将促进癌症的临床治疗。在临床开发中需要结合碳水化合物作为靶向基团和pH敏感的可裂解连接基的双功能前药。在这里，使用了合格的N-苯基氨基甲酸酯-d-葡萄糖基氢氧嘧啶-1,5-内酰胺结构，并被证明是药物设计中潜在的候选药物。为了证明这一概念，在酸性条件下模拟溶酶体的HPLC和LC-MS证实了贝克曼重排和降解产物的可能机制。因此，以感兴趣的药物制备的作为前药载体的d-葡萄糖基羟基肟-1,5-内酰胺的策略将为化学疗法提供巨大的潜在途径。