Drawbaugh R, Bouffard C, Strauss M
J Med Chem. 1976 Nov;19(11):1342-5. doi: 10.1021/jm00233a019.
A series fo prodrug modifications of 6-mercaptopurine (6-MP) containing dinitrobenzoate ester moieties with varying chain length has been prepared. These compounds were shown to be cytotoxic in several cell culture screens and also exhibited significant activity against L1210 lymphoid leukemia in vivo. The possibility exists that the transport and distribution of these compounds in vivo will be determined, in part, by increased lipophilic character, with a consequent selective localization in lymphatic and CNS tissue.
已制备了一系列含有不同链长二硝基苯甲酸酯部分的6-巯基嘌呤（6-MP）前药修饰物。这些化合物在多个细胞培养筛选中显示出细胞毒性，并且在体内对L1210淋巴细胞白血病也表现出显著活性。有可能这些化合物在体内的转运和分布部分将由增加的亲脂性决定，从而导致在淋巴组织和中枢神经系统组织中的选择性定位。
