Schwabe K, Wohlrab W
Zentralinstitut für Krebsforschung der Akademie der Wissenschaften, DDR, Berlin-Buch.
Pharmazie. 1988 Aug;43(8):521-3.
Using two sources of selection, the higher beta-glucuronidase and tyrosinase content of malignant melanomas, new transport forms are synthetized, which are toxified to quinoids, cytotoxic products by the above mentioned enzymes. These transport forms selectively inhibit the growth of melanomas. For instance, 4-methylcatechol-2-O-beta-D-glucopyranosiduronic acid (3) is synthetized by the reaction of 4-methylcatechol with tetra-O-acetyl-beta-D-glucopyranosiduronic acid methyl ester in the presence of p-toluenesulfonic acid following treatment with alkali. 3 inhibits the growth of B16 melanoma of the mouse significantly.
利用两种筛选来源，恶性黑色素瘤中较高的β - 葡萄糖醛酸酶和酪氨酸酶含量会合成新的转运形式，这些转运形式会被上述酶氧化为醌类细胞毒性产物。这些转运形式可选择性抑制黑色素瘤的生长。例如，4 - 甲基邻苯二酚 - 2 - O - β - D - 吡喃葡萄糖醛酸（3）是在对甲苯磺酸存在下，4 - 甲基邻苯二酚与四 - O - 乙酰 - β - D - 吡喃葡萄糖醛酸甲酯反应后经碱处理合成的。3能显著抑制小鼠B16黑色素瘤的生长。
