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Original scientific paper

https://doi.org/10.5562/cca3531

Synthesis and Antiproliferative activity in vitro of Amidino Substituted 2-phenylbenzazoles

Livio Racané ; Department of Applied Chemistry, Faculty of Textile Technology, University of Zagreb, Baruna Filipovića 28a, HR-10000 Zagreb, Croatia
Kristina Butković ; Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Marulićev trg 20, HR-10000 Zagreb, Croatia
Irena Martin-Kleiner ; Division of Molecular Medicine, Ruđer Bošković Institute, Bijenička cesta 54, P. O. Box 180, HR-10000 Zagreb, Croatia
Marijeta Kralj ; Division of Molecular Medicine, Ruđer Bošković Institute, Bijenička cesta 54, P. O. Box 180, HR-10000 Zagreb, Croatia
Grace Karminski-Zamola ; Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Marulićev trg 20, HR-10000 Zagreb, Croatia
Marijana Hranjec ; Department of Organic Chemistry, Faculty of Chemical Engineering and Technology, University of Zagreb, Marulićev trg 20, HR-10000 Zagreb, Croatia


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Abstract

Within this work we describe the synthesis of versatile substituted 2-phenyl benzothiazole 3–10 and 2-phenylbenzimidazole 12–19 derivatives bearing amidino groups. Furthermore, the synthesized compounds were explored for their antiproliferative activity in vitro on three cancer cell lines. Tested compounds showed moderate to strong antiproliferative activity. Furthermore, the type of the attached amidino group on benzazole nuclei has the significant impact on the antiproliferative activity only within benzimidazole derivatives with 2-imidazolinyl substituted derivatives being more active in comparison to amidino substituted analogues. All obtained results revealed that this type of benzothiazole derivatives have a great potential for further optimization and development of more efficient potential antiproliferative agents.

This work is licensed under a Creative Commons Attribution 4.0 International License.

Keywords

amidines; benzimidazoles; benzothiazoles; antiproliferative activity in vitro

Hrčak ID:

227007

URI

https://hrcak.srce.hr/227007

Publication date:

29.7.2019.

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