2. Academic Validation
  3. Synthesis of novel C4-benzazole naphthalimide derivatives with potent anti-tumor properties against murine melanoma

Synthesis of novel C4-benzazole naphthalimide derivatives with potent anti-tumor properties against murine melanoma

  • Bioorg Med Chem. 2017 Jan 15;25(2):789-794. doi: 10.1016/j.bmc.2016.11.057.
Yen-Ta Lu 1,  Tien-Ling Chen 2,  Kuo-Song Chang 3,  Chia-Ming Chang 4,  Tsai-Yin Wei 4,  Jen-Wei Liu 5,  Chih-Ang Hsiao 5,  Tzenge-Lien Shih 6
Affiliations

Affiliations

  • 1 Chest Division, Medical Department, MacKay Memorial Hospital, Zhongshan Dist., 10449 Taipei, Taiwan.
  • 2 Division of Allergy, Immunology and Rheumatology, Department of Internal Medicine, MacKay Memorial Hospital, Zhongshan Dist., 10449 Taipei, Taiwan.
  • 3 Department of Emergency Medicine, MacKay Memorial Hospital, Zhongshan Dist., 10449 Taipei, Taiwan; Department of Medicine, MacKay Medical College, New Taipei City 25245, Taiwan.
  • 4 Department of Medical Research, MacKay Memorial Hospital, Tamsui Dist., 25173 New Taipei City, Taiwan.
  • 5 Department of Chemistry, Tamkang University, Tamsui Dist., 25137 New Taipei City, Taiwan.
  • 6 Department of Chemistry, Tamkang University, Tamsui Dist., 25137 New Taipei City, Taiwan. Electronic address: tlshih@mail.tku.edu.tw.
PMID: 27939348 DOI: 10.1016/j.bmc.2016.11.057
Abstract

Novel C4-benzazole naphthalimide derivatives were synthesized and tested in vitro and in vivo as anti-cancer drugs. Among these synthetic molecules, compounds 9 and 10 exhibited cytotoxicity against murine B16F10 melanoma cells. In addition, the above-mentioned compounds significantly suppressed lung tumor metastasis with no visible sign of toxicity.

Keywords

B16F10 cells; Benzazole; MTS assay; Melanoma; Naphthalimide; Topoisomerase II.

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