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Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents. 2005
Masao Yoshida, and
Ichiro Hayakawa, and
Noriyuki Hayashi, and
Toshinori Agatsuma, and
Youko Oda, and
Fumie Tanzawa, and
Shiho Iwasaki, and
Kumiko Koyama, and
Hidehiko Furukawa, and
Shinichi Kurakata, and
Yuichi Sugano
Medicinal Chemistry Research Laboratories, Sankyo Co. Ltd., Shinagawa-ku, Tokyo 140-8710, Japan.
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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