Synthesis and Antiproliferative Activity of Cyano and Amidino Substituted 2-Phenylbenzothiazoles |
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Authors: | Livio Racanè Vesna Trali?-Kulenovi? Richard P Kitson Grace Karminski-Zamola |
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Institution: | (1) Department of Applied Chemistry, Faculty of Textile Technology, University of Zagreb, Zagreb, Croatia;(2) Department of Molecular Biology and Immunology, University of North Texas Health Science Center, Fort Worth, TX, USA;(3) Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Zagreb, Croatia |
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Abstract: | Summary. Series of cyano, dicyano, amidino, and diamidino substituted 2-phenylbenzothiazoles were prepared. Mono- and dicyano substituted
benzothiazoles were obtained by condensation of appropriate substituted benzaldehydes with 2-aminothiophenol or 4-amino-3-mercaptobenzonitrile.
The appropriate amidines or diamidines were prepared by Pinner reaction. The compounds were tested against breast, prostate, and lung cancer cell lines in a 72 h cytotoxicity assay. Many
of the compounds had at 10 μM activity equivalent to 2-(4-aminophenyl)benzothiazole, while four compounds had significantly better activity, particularly
in the breast cancer model. |
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Keywords: | , Heterocycles, Benzothiazoles, Amidines, Antitumor agents, Structure-activity relationship, |
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