Synthesis and cytotoxicity of 1,6,8,9-substituted α-carboline derivatives.
α-Carboline (pyrido[2,3-b]indole) was selected as the basic scaffold for development of antileukemic agents by structural modification. From the structure-activity study, it was found that sequential introduction of 6-acetyl and 9-substituted benzyl groups onto an α-Carboline scaffold resulted in 6-acetyl-9-(3,5-dimethoxybenzyl)-9H-pyrido[2,3-b]indole and 6-acetyl-9-(3,4,5-trimethoxybenzyl)-9H-pyrido[2,3-b]indole with potent cytotoxicity against the HL-60 cell line. These two compounds will be used as new lead compounds for further investigation.
China Medical University, Taichung, Taiwan.
Jui-Ying
JY
Tsai
Yi-Chien
YC
Lin
Mei-Hua
MH
Hsu
Sheng-Chu
SC
Kuo
Li-Jiau
LJ
Huang
D002243:Carbolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity*; D002453:Cell Cycle / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D018922:HL-60 Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D002243:Carbolines; C055571:alpha-carboline