Synthesis and Cytotoxicity of 1,6,8,9‐Substituted α‐Carboline Derivatives

The Kaohsiung Journal of Medical Sciences - Tập 26 - Trang 593-602 - 2010
Jui-Ying Tsai1, Yi-Chien Lin1, Mei-Hua Hsu1, Sheng-Chu Kuo1, Li-Jiau Huang1
1Graduate Institute of Pharmaceutical Chemistry, College of Pharmacy, China Medical University, Taichung, Taiwan

Tóm tắt

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.


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