Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents

✍ Scribed by Masao Yoshida; Ichiro Hayakawa; Noriyuki Hayashi; Toshinori Agatsuma; Youko Oda; Fumie Tanzawa; Shiho Iwasaki; Kumiko Koyama; Hidehiko Furukawa; Shinichi Kurakata; Yuichi Sugano

• Book ID: 108073687
• Publisher: Elsevier Science
• Year: 2005
• Tongue: English
• Weight: 259 KB
• Volume: 15
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2005.05.077

✦ Synopsis

Based on 2-methyl-4-nitro-2H-pyrazole-3-carboxylic acid[2-(cyclohexanecarbonylamino)benzothiazol-6-yl]amide (1), which shows selective cytotoxicity against tumorigenic cell lines, 2,6-dichloro-N-[2-(cyclopropanecarbonylamino)benzothiazol-6yl]benzamide (13b) was designed and synthesized as a biologically stable derivative containing no nitro group. The highly potent derivative 13b exhibited excellent in vivo inhibitory effect on tumor growth.