Tam M N, Nam N H, Jin G Z, Ahn B Z
College of Pharmacy, Chungnam National University, Taejon, Korea.
Arch Pharm Res. 2000 Aug;23(4):283-7. doi: 10.1007/BF02975436.
A series of 2-(1-hydroxyiminoalkyl)-1,4-dimethoxy-9,10-anthraquinones (oximes) was synthesized and evaluated for cytotoxicity against L1210 cells and A549 cells. These oximes showed a greater cytotoxic activity compared to those of 2-(1-hydroxyalkyl)-1,4-dimethoxy-9,10-anthraquinones as the hydroxyalkyl bioisosteres. The enhanced cytotoxicity assumed to be due to the improved water solubility of the hydroxyimino group. Moreover, it was found that the cytotoxicity of the oximes decreased with elongation of alkyl groups at the side chain. All of the synthesized compounds showed higher cytotoxicity against L1210 cells than A549 cells.
合成了一系列2-(1-羟基亚氨基烷基)-1,4-二甲氧基-9,10-蒽醌（肟），并评估了它们对L1210细胞和A549细胞的细胞毒性。与作为羟烷基生物电子等排体的2-(1-羟烷基)-1,4-二甲氧基-9,10-蒽醌相比，这些肟表现出更大的细胞毒性活性。增强的细胞毒性被认为是由于羟基亚氨基基团的水溶性提高所致。此外，发现肟的细胞毒性随着侧链烷基的延长而降低。所有合成化合物对L1210细胞的细胞毒性均高于对A549细胞的细胞毒性。
