作为强效抗肿瘤剂的苯并噻唑衍生物的合成与生物学评价
Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents.
作者信息
Yoshida Masao, Hayakawa Ichiro, Hayashi Noriyuki, Agatsuma Toshinori, Oda Youko, Tanzawa Fumie, Iwasaki Shiho, Koyama Kumiko, Furukawa Hidehiko, Kurakata Shinichi, Sugano Yuichi
机构信息
Medicinal Chemistry Research Laboratories, Sankyo Co. Ltd., Shinagawa-ku, Tokyo 140-8710, Japan.
出版信息
Bioorg Med Chem Lett. 2005 Jul 15;15(14):3328-32. doi: 10.1016/j.bmcl.2005.05.077.
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.
基于对致瘤细胞系具有选择性细胞毒性的2-甲基-4-硝基-2H-吡唑-3-羧酸[2-(环己烷羰基氨基)苯并噻唑-6-基]酰胺(1)，设计并合成了无硝基的生物稳定衍生物2,6-二氯-N-[2-(环丙烷羰基氨基)苯并噻唑-6-基]苯甲酰胺(13b)。高效衍生物13b对肿瘤生长表现出优异的体内抑制作用。
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