文章基本信息

标题：Design and synthesis of novel thiophenecarbohydrazide,thienopyrazole and thienopyrimidine derivatives as antioxidant and antitumor agents
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作者：AMEEN ALI ABU-HASHEM ; MOHAMED FATHY EL-SHEHRY ; FARID ABD-ELRAHEEM BADRIA 等
期刊名称：Acta Pharmaceutica
电子版ISSN：1846-9558
出版年度：2010
卷号：60
期号：3
页码：311-323
DOI：10.2478/v10007-010-0027-6
语种：English
出版社：Sciendo
摘要：Amino-5-acetyl-4-methyl-thiophene-3-carboxylic acid ethyl ester (1) and 5-acetyl-2-amino-4-methylthiophene- -3-carbohydrazide (2) were synthesized and used as starting materials for the synthesis of new series of 1-(5- -amino-4-(3,5-dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2-yl) ethanone (3a),1-(5-amino-4-(4-chloro-3,5- -dimethyl-1H-pyrazole-1-carbonyl)-3-methylthiophen-2- -yl) ethanone (3b),1-(4-methyl-2-amino-5-acetylthiophene-3-carbonyl)pyrazolidine-3,5-dione (4),(Z)-N'-(4 -methyl-2-amino-5-acetylthiophene-3-carbonyl) formohydrazonic acid (5a),(Z)-ethyl-N'-4-methyl-2-amino-5- -acetylthiophene-3-carbonylformo hydrazonate (5b),6- -acetyl-3-amino-2,5-dimethylthieno[2,3-d]pyrimidin-4(3H)- -one (8),5-methyl-3-amino-2-mercapto-6-acetylthieno [2,3-d]pyrimidin-4(3H)-one (10) and 5-methyl-6-acetyl-2- -thioxo-2,3-dihydrothieno[2,3-d]pyrimidin-4(1H)-one (12) as potential antioxidant and antitumor agents.Pharmacological tests showed that compounds 6a,6b,8,10 and 12 exhibited significant antitumor and antioxidant activity.
关键词：thienopyrazole;thieno[2;3-d]pyrimidines;thiophenecarbohydrazide;antioxidant activity;bleomycin- -dependent DNA damage;antitumor activity