Antitumour benzothiazoles. Part 20: 3'-cyano and 3'-alkynyl-substituted 2-(4'-aminophenyl)benzothiazoles as new potent and selective analogues.
The synthesis of a new series of antitumour 2-(4-aminophenyl)benzothiazole analogues, substituted in the 3'-position by cyano or alkynyl groups, is described. Several of the analogues, notably the 5-fluorinated compounds 7c and 9c, were found to possess potent in vitro activity against MCF-7 and MDA 468 human cancer cell lines. More comprehensive in vitro analysis (NCI 60-cell line) established compound 7c as a particularly potent and selective 2-(4-aminophenyl)benzothiazole analogue.
Hutchinson
Ian
I
Cancer Research Laboratories, School of Pharmaceutical Sciences, University of Nottingham, Nottingham NG7 2RD, UK.
Bradshaw
Tracey D
TD
Matthews
Charles S
CS
Stevens
Malcolm F G
MF
Westwell
Andrew D
AD
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D052160:Benzothiazoles; D006801:Humans; D007202:Indicators and Reagents; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
C111133:2-(4-aminophenyl)benzothiazole; D000970:Antineoplastic Agents; D052160:Benzothiazoles; D007202:Indicators and Reagents; D013844:Thiazoles