Weimar C, von Angerer S, Wiegrebe W
Institute of Pharmacy and Sonderforschungsbereich 234, University of Regensburg, Germany.
Arch Pharm (Weinheim). 1991 Aug;324(8):509-18. doi: 10.1002/ardp.2503240810.
Most of the methoxy-8H-dibenzo[a,g]isoquinolin-8-ones 3a-h and their acetoxy derivatives 6a-e were synthesized by condensation of 1-oxo-1,2,3,4-tetrahydroisoquinolines 4a-c and homophthalic acid anhydrides 5a and b, ether cleavage and acetylation. These protoberberinones were tested for cytostatic activity in vitro using MDA-MB-231 mammary tumor cells and for interaction with native calf thymus DNA. Tetramethoxy-8-oxoberbine 3f shows an inhibition of cell proliferation of 87% at a concentration of 10(-5) mole; its cytostatic effect does not depend on intercalation into DNA.
大多数甲氧基 - 8H - 二苯并[a,g]异喹啉 - 8 - 酮3a - h及其乙酰氧基衍生物6a - e是通过1 - 氧代 - 1,2,3,4 - 四氢异喹啉4a - c与高邻苯二甲酸酐5a和b缩合、醚键裂解和乙酰化反应合成的。使用MDA - MB - 231乳腺肿瘤细胞对这些原小檗碱酮进行了体外细胞抑制活性测试，并测试了它们与天然小牛胸腺DNA的相互作用。四甲氧基 - 8 - 氧代小檗碱3f在浓度为10(-5)摩尔时显示出87%的细胞增殖抑制率；其细胞抑制作用不依赖于插入DNA。
