新型噻吩甲酰肼、噻吩吡唑和噻吩嘧啶衍生物的设计与合成及其抗氧化和抗肿瘤活性。
Design and synthesis of novel thiophenecarbohydrazide, thienopyrazole and thienopyrimidine derivatives as antioxidant and antitumor agents.
机构信息
Photochemistry Department (Heterocyclic Unit), National Research Center, 12622 Dokki, Giza, Egypt.
出版信息
Acta Pharm. 2010 Sep;60(3):311-23. doi: 10.2478/v10007-010-0027-6.
2-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.
2-氨基-5-乙酰基-4-甲基噻吩-3-羧酸乙酯（1）和 5-乙酰基-2-氨基-4-甲基噻吩-3-甲酰肼（2）被合成，并用作合成一系列新的 1-（5-氨基-4-（3,5-二甲基-1H-吡唑-1-羰基）-3-甲基噻吩-2-基）乙酮（3a）、1-（5-氨基-4-（4-氯-3,5-二甲基-1H-吡唑-1-羰基）-3-甲基噻吩-2-基）乙酮（3b）、1-（4-甲基-2-氨基-5-乙酰基噻吩-3-甲酰基）吡唑烷-3,5-二酮（4）、（Z）-N' -（4-甲基-2-氨基-5-乙酰基噻吩-3-甲酰基）甲脒（5a）、（Z）-乙基-N'-4-甲基-2-氨基-5-乙酰基噻吩-3-甲酰基甲脒（5b）、6-乙酰基-3-氨基-2,5-二甲基噻吩并[2,3-d]嘧啶-4(3H)-酮（8）、5-甲基-3-氨基-2-巯基-6-乙酰基噻吩并[2,3-d]嘧啶-4(3H)-酮（10）和 5-甲基-6-乙酰基-2-硫代-2,3-二氢噻吩并[2,3-d]嘧啶-4(1H)-酮（12）作为潜在的抗氧化和抗肿瘤药物。药理试验表明，化合物 6a、6b、8、10 和 12 表现出显著的抗肿瘤和抗氧化活性。
Zotero 插件