Synthesis and in vitro cytotoxicity of haloderivatives of noscapine

• DOI: 10.1016/j.bmc.2006.05.069
• Publication Date: 2006-06-20T11:31:42Z
• Authors: Akhilesh Kumar Verma; Sandhya Bansal; Jaspal Singh; Rakesh Kumar Tiwari; V. Kasi Sankar; Vibha Tandon; Ramesh Chandra
• Keywords: Noscapine; 0301 basic medicine; Brain Neoplasms; Cell Survival; Tetrazolium Salts; Antineoplastic Agents; 3. Good health; Kinetics; Thiazoles; 03 medical and health sciences; Cell Line, Tumor; Humans; Indicators and Reagents; Glioblastoma; Cell Proliferation

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 microM 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 microM) 9-bromonoscapine (46.7%) and 9-chloronoscapine (45.7%) did not show any significant difference.