Bioorganic & Medicinal Chemistry Letters 2005-07-15

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

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

Index: Bioorg. Med. Chem. Lett. 15(14) , 3328-32, (2005)

Full Text: HTML

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.