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Synthesis and in vitro cytotoxicity of haloderivatives of noscapine

Authors
Journal
Bioorganic & Medicinal Chemistry
0968-0896
Publisher
Elsevier
Publication Date
Volume
14
Issue
19
Identifiers
DOI: 10.1016/j.bmc.2006.05.069
Keywords
  • Synthesis
  • Noscapine
  • Halo-Noscapine
  • U-87 Glioblastoma Cell Line
  • Cell Proliferation

Abstract

Abstract Three haloderivatives of noscapine 2– 4 were synthesized chemoselectively and their in vitro cytotoxicity was assessed by MTT assay on U-87 human glioblastoma cell lines. At 50 μM concentration after 72 h, 9-chloronoscapine 2, 9-bromonoscapine 3 (EM011), and 9-iodonoscapine 4 killed 87.8%, 51.2%, and 56.8% cells, respectively, however noscapine kills only 40% of the cells; revealing 9-chloronoscapine as a potential cytotoxic agent than noscapine and 9-bromonoscapine (EM011). At low concentration (1 μM) 9-bromonoscapine (46.7%) and 9-chloronoscapine (45.7%) did not show any significant difference.

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