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Updated: Aug 17, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents
Masao Yoshida1, Ichiro Hayakawa, Noriyuki Hayashi
1Medicinal Chemistry Research Laboratories, Sankyo Co. Ltd., Shinagawa-ku, Tokyo 140-8710, Japan.
Abstract:
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-6-yl]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.
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