📜4-Nitrophthalic Acid Diethyl Ester置于盐酸,氢氧化钾,羟胺体系中,用 甲醇,乙醇 用作溶剂,以68%的收率获得n-羟基-4-硝基邻苯二甲酰亚胺
参考文献:Synthesis,Biological Evaluation,And Quantitative Structure-Activity Relationship Analysis Of 2-Hydroxy-1H-Isoindolediones As New Cytostatic Agents
标题:Synthesis,Biological Evaluation,And Quantitative Structure-Activity Relationship Analysis Of 2-Hydroxy-1H-Isoindolediones As New Cytostatic Agents
摘要:A Series Of 16 Derivatives Of 2-Hydroxy-1H-Isoindole-1,3-Diones Was Designed And Synthesized As Potential Antitumor Agents. The Cytostatic Activity Against L1210 Cell Growth Of These Compounds Was Studied,And Their Ic50 Values Were Found To Be In The Range Of 10(-4) To 10(-8) M. Quantitative Structure-Activity Relationship Analysis Of These Compounds Showed That The Inhibitory Effect Was Well Correlated With The Electronic And The Lipophilic Parameters. Derivatives Having A Substituent With Strongly Electron-Donating Properties At The 6-Position Showed Enhanced Inhibitory Activity While Compounds Having An Electron-Withdrawing Group At The Same Position Showed Lower Activity.
Doi:10.1021/jm00386A012