Synthesis and Biological Evaluation of Some Substituted-2-N-(5-chloro-2-methoxy-4-methylphenylsulphonyl) Glutamic Acid Derivatives against Prostate Cancer Cell Line PC3

• Hassan Ghaneya Sayed

  Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University

• Abdel Rahman Doaa Ezzat

  Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University

書誌事項

タイトル別名

• Synthesis and Biological Evaluation of Some Substituted-2-<i>N</i>-(5-chloro-2-methoxy-4-methylphenylsulphonyl) Glutamic Acid Derivatives against Prostate Cancer Cell Line PC3

抄録

New series of substituted glutamine 5a–l and glutamic acid diamides, diureide and dihydrazide 7a–e were synthesized from parent glutamic acid compound 3 and evaluated for their cytotoxic activity against tumor cell line PC3 (prostate cancer cell line). Most of the tested compounds exploited potent growth inhibitory activity with IC₅₀ values ranging 0.034–3.97 µM. Particularly, compounds 5a, 3, 5j, 5b, 7c, 7e, 5l, and 5k exhibited superior potency (IC₅₀=0.034, 0.04, 0.05, 0.074, 0.25, 0.4, 0.49, 0.522 µM, respectively) to the reference drug Doxorubicin (IC₅₀=0.63 µM), while compound 7b showed IC₅₀, 0.71 µM, comparable to that of Doxorubicin. In summary, the newly synthesized compounds provided promising new lead for the future design and development of glutamine and glutamic acid derivatives as novel antitumor agents. The quantitative structure–activity relationship (QSAR) study was applied to find a mathematical correlation between the structures of compounds and their activity against PC3 cell line expressed as IC₅₀ values.

収録刊行物

• ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ

  ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 61 (2), 212-221, 2013

  公益社団法人 日本薬学会

キーワード

• glutametergic system
• glutamic acid
• glutamine
• prostate cancer (PC)
• PC3 cell line

詳細情報

• CRID: 1390282679154825088
• NII論文ID: 130003360728
• NII書誌ID: AA00602100
• DOI: 10.1248/cpb.c12-00881
• COI: 1:STN:280:DC%2BC3szksVemug%3D%3D
• ISSN: 13475223
• ISSN: 00092363
• NDL書誌ID: 024220398
• PubMed: 23370196
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I024220398
• Web Site: https://www.jstage.jst.go.jp/article/cpb/61/2/61_c12-00881/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2013228919
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可