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Merck

Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents.

Bioorganic & medicinal chemistry letters (2005-06-16)
Masao Yoshida, Ichiro Hayakawa, Noriyuki Hayashi, Toshinori Agatsuma, Youko Oda, Fumie Tanzawa, Shiho Iwasaki, Kumiko Koyama, Hidehiko Furukawa, Shinichi Kurakata, Yuichi Sugano
RESUMO

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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Sigma-Aldrich
2-Amino-6-nitrobenzothiazole, ≥97%