title: Synthesis and biological evaluation of benzothiazole derivatives as potent antitumor agents.
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.
authors.affiliation: Medicinal Chemistry Research Laboratories, Sankyo Co. Ltd., Shinagawa-ku, Tokyo 140-8710, Japan.
authors.forename: Masao
authors.initials: M
authors.lastname: Yoshida
authors.forename: Ichiro
authors.initials: I
authors.lastname: Hayakawa
authors.forename: Noriyuki
authors.initials: N
authors.lastname: Hayashi
authors.forename: Toshinori
authors.initials: T
authors.lastname: Agatsuma
authors.forename: Youko
authors.initials: Y
authors.lastname: Oda
authors.forename: Fumie
authors.initials: F
authors.lastname: Tanzawa
authors.forename: Shiho
authors.initials: S
authors.lastname: Iwasaki
authors.forename: Kumiko
authors.initials: K
authors.lastname: Koyama
authors.forename: Hidehiko
authors.initials: H
authors.lastname: Furukawa
authors.forename: Shinichi
authors.initials: S
authors.lastname: Kurakata
authors.forename: Yuichi
authors.initials: Y
authors.lastname: Sugano
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D001549:Benzamides / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D005260:Female; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy*; D051379:Mice; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D013997:Time Factors; D023041:Xenograft Model Antitumor Assays
chemical_list: C506243:2,6-dichloro-N-(2-(cyclopropanecarbonylamino)benzothiazol-6-yl)benzamide; D000970:Antineoplastic Agents; D001549:Benzamides; D052160:Benzothiazoles; D013844:Thiazoles; C005465:benzothiazole