靛玉红肟甲醚的合成及构效关系的研究

STUDIES ON SYNTHESIS AND STRUCTURE-ACTIVITY RELATIONSHIP OF INDIRUBIN MONOXIME METHYL ETHER

目的：研究靛玉红肟甲醚的合成及构效关系。方法：用靛玉红、NH2OH·HCL、CH3I在乙醇中直接合成靛玉红肟甲酸并得到其晶体；用FT-IR170SX光谱法、JEDL－JNM－FX90Q，HNMR光谱法、CarloErba1106元素分析法、CAD4衍射法是靛玉红肟甲醚分子结构和晶体结构；用美兰试验测抗白血病活性。结果：测定出靛玉红肟甲醚的分子结构和晶体结构，并得出靛玉红肟甲醚的抗白血病活性优于靛玉红。结论：肟甲醚结构＞C＝N－OCH3对靛玉红类药物抗白血病活性有重要作用，对寻找这类新药有重要意义。

Objective: To study the synthesis and structure-activity relationship of indirubin monooxime methyl ether(IMME). Methods: IMME was synthesized with mdirubin, methyl iodine and aminohydrin hydrochloride in alcohol and its crystalline was obtained; the molecular and crystalline structures of IMME was determined by FT-IR 170SX spectroscopy, JEDL-JNM-FX90Q-HNMR spectroscopy, Carlo Erba-1106 ultimate analysis and CAD4 diffraction;the antileukemic activity of IMME was determined by methylene blue method. Results: The molecular and crystalline structures of IMME were determined and the antileukemic achvity of IMME was found better than that of indirubin. Con-clusion: The Structure of monooxime mehyl ether(>C=N-OCH3) is impotant to antileukemic activity of indirubins,which has imporant significance in finding new drugs of this sort.