Potent anticancer and antimicrobial activities of pyrazole, oxazole and pyridine derivatives containing 1,2,4-triazine moiety

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• 作者：Amira S. Abd El-All ; Souad A. Osman ; Hanaa M. F. Roaiah…
• 关键词：1 ; 2 ; 4 ; Triazine ; Chalcone derivatives ; Furochromone ; Pyrazolines ; Oxazoles ; Cyanopyridines ; Cytotoxicity ; Anticancer activity ; Antimicrobial activity
• 刊名：Medicinal Chemistry Research
• 出版年：2015
• 出版时间：December 2015
• 年：2015
• 卷：24
• 期：12
• 页码：4093-4104
• 全文大小：706 KB
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• 作者单位：Amira S. Abd El-All (1)
  Souad A. Osman (2)
  Hanaa M. F. Roaiah (1)
  Mohamed M. Abdalla (3)
  Abeer A. Abd El Aty (1)
  Wafaa H. AbdEl-Hady (2)
  
  1. Research Division of Pharmaceutical and Drug Industries, Department of Natural and Microbial Product, National Research Center, El-Behoos Street, Dokki, Giza, 12622, Egypt
  2. Division of Inorganic Chemical Industries and Mineral Resources, Department of Organometallic and Organometalloid Chemistry, National Research Center, El-Behoos Street, Dokki, Giza, 12622, Egypt
  3. Research Unit, Saco Pharm. Co., 6 October City, 11632, Egypt
  
• 刊物主题：Pharmacology/Toxicology; Biochemistry, general; Cell Biology;
• 出版者：Springer US
• ISSN：1554-8120

文摘

Due to the importance of biological activities of 1,2,4-triazine derivatives, in this manuscript, ten of newly synthesized compounds containing 1,2,4-triazine moiety were prepared. Anticancer and antimicrobial activities of some selected synthesized compounds were screened. Chalcone derivatives 6, 7 were synthesized via reaction of Mannich base 2 in acetic acid and fused sodium acetate with formyl khellin 5 or vanillin. Treatment of chalcone derivatives 6, 7 toward hydrazine hydrate, phenyl hydrazine, hydroxylamine hydrochloride or malononitrile, respectively, led to give pyrazoline 8, 9, 10, 11, oxazole 12, 13 and pyridine 14, 15 derivatives, respectively. The structures of the isolated products were established by elementary analysis and spectral data studies. Compounds 1, 5, 6, 8, 10, 12 and 14 were tested against different human cancer cell lines, and cytotoxicity in vitro and most of the synthesized compounds were proved to have high activities against cytotoxic test. Then, the compounds 1, 5, 6, 8, 10, 12 and 14 were tested against cancer in vivo, and the result was established. Also, antimicrobial activity of compounds 1, 5, 6, 8, 10, 12 and 14 was screened in vitro against a panel of gram-positive and gram-negative bacterial pathogens and fungi. The results indicated that compound 5 showed higher antimicrobial activity than compounds 1, 6, 8, 10, 12 and 14, and compound 5 exhibited a wide range of antimicrobial activities against gram-positive and gram-negative bacteria and fungi, greater than well-known antibacterial and antifungal agents with minimal inhibitory concentration ranged between 6.25 and 25 μg. Keywords 1,2,4-Triazine Chalcone derivatives Furochromone Pyrazolines Oxazoles Cyanopyridines Cytotoxicity Anticancer activity Antimicrobial activity