Papot S, Combaud D, Gesson J P
Laboratoire de Chimie 12, Université de Poitiers et CNRS, Poitiers, France.
Bioorg Med Chem Lett. 1998 Sep 22;8(18):2545-8. doi: 10.1016/s0960-894x(98)00454-5.
A new glucuronylated prodrug of doxorubicin, potentially useful for ADEPT or PMT cancer chemotherapy, has been prepared from 4-methyl phenyl malonaldehyde. The enol ether spacer, linked via a carbamate to the 3'-amino group of doxorubicin is rapidly cleaved after beta-glucuronidase (E coli) catalyzed hydrolysis at pH 7.2 and 37 degrees C.
一种新的阿霉素葡萄糖醛酸化前药已由4-甲基苯基丙二醛制备而成，它可能对抗体导向酶解前药疗法（ADEPT）或前体药物疗法（PMT）的癌症化疗有用。通过氨基甲酸酯连接到阿霉素3'-氨基上的烯醇醚间隔基，在pH 7.2和37摄氏度下经β-葡萄糖醛酸酶（大肠杆菌）催化水解后会迅速裂解。
