Design, synthesis and biological evaluation of novel thiophene and theinopyrimidine derivatives as anticancer agents

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• 作者：Madlen B. Labib ; Phoebe F. Lamie
• 关键词：Thiophene ; Thienopyrimidine ; HepG2 ; Anticancer agents
• 刊名：Medicinal Chemistry Research
• 出版年：2016
• 出版时间：November 2016
• 年：2016
• 卷：25
• 期：11
• 页码：2607-2618
• 全文大小：872 KB
• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120
• 卷排序：25

文摘

Some novel thiophene and theinopyrimidine derivatives have been synthesized. Their structures were confirmed by elemental analyses, infrared, 1H NMR, 13C NMR and mass spectral data. All the target compounds were screened against liver adenocarcinoma (HepG2) cell line. Compounds 9c, 9b, 10b, and 7c in a sequent were the most potent compounds between all the test compounds with IC₅₀ values [0.01063, 0.01158, 0.01729, 0.01957 µM], respectively. Compounds 13b, 7b, 5d, 9a, 8a, and 11b showed higher activity with IC₅₀ values ranged from 0.02231 to 0.03673 µM when compared with 5-flurouracil (A) as a reference drug (IC₅₀ = 0.0384 µM).