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
  • 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: [email protected].
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.