Bai Shu-fang
2011
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Quality indicators
Journal
Journal of Tianjin Medical University
Abstract
Objective:To obtain compounds with superior antitumor bioactivity and overcoming multidrug resistance.Methods: The 5-methoxyindole was reacted with alkyl chlorides or acyl chlorides to get N-substituted 5-methoxy-indoles.N-substituted 5-methoxyindol-3-ylglyoxyl chlorides were prepared by the reaction of various N-substituted 5-methoxyindoles with oxalyl chloride.Subsequently,it was coupled with 4-amino-4'-demethylepipodophyllotoxin in the presence of triethylamine to generate the products.HeLa cell line was used to assess the cytotoxicity of these compounds in vitro.Results: Through the oxalyl bridge indoles and success split joint podophyllotoxin,and 8 novel podophyllotoxin derivatives were synthesized.Conclusion:Part of the eight compounds which are sythesised show favourable antitumor activities,and some compounds(7a,7b) show comparable antitumor activities to that of etoposide.