Synthesis, cytotoxicity and toxicity of thieno[2,3-d]pyrimidine derivatives derived from 2-amino-3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophene

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• 作者：Mahmoud A. Abdelaziz ; Hend M. El-Sehrawi ; Rafat M. Mohareb
• 关键词：Tetrahydrobenzo[b]thiophene ; Thieno[2 ; 3 ; d]pyrimidine ; Cyanomethylene ; Cytotoxicity
• 刊名：Medicinal Chemistry Research
• 出版年：2015
• 出版时间：November 2015
• 年：2015
• 卷：24
• 期：11
• 页码：3932-3948
• 全文大小：834 KB
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• 作者单位：Mahmoud A. Abdelaziz (1)
  Hend M. El-Sehrawi (2)
  Rafat M. Mohareb (3)
  
  1. Department of Chemistry, Faculty of Science, University of Tabuk, P. O. Box 741, Tabuk, 71491, Kingdom of Saudi Arabia
  2. Pharmaceutical Chemistry Department, Faculty of Pharmacy (Girls), Al-Azhar University, Nasr City, Cairo, Egypt
  3. Department of Chemistry, Faculty of Science, Cairo University, Giza, Egypt
  
• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120

文摘

The 4,5,6,7-tetrahydrobenzo[b]thiophene derivative 1 reacted with benzoylisothiocyanate to give N-benzoylthiourea derivative 3. The latter underwent ready cyclization to give the tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivative 4 which was used as the key starting compound for a series of heterocyclization reactions to produce thiophene, pyridine, pyrimidine and pyran derivatives. The cytotoxicity of the newly synthesized products was evaluated using six cancer and one normal cell lines. The toxicity of compounds with the optimal cytotoxicity was measured using shrimp larvae. Keywords Tetrahydrobenzo[b]thiophene Thieno[2,3-d]pyrimidine Cyanomethylene Cytotoxicity