engleski

Antiproliferative activity of amidino substituted benzimidazoles and benzothiazoles explored by 2D and 3D cell culture system

It is well known that amidines are structural parts of numerous compounds of biological interest including important medical and biochemical agents. Amidine substituents placed at the termini of the molecule have great importance in the molecule - biological target interactions allowing the formation of the stable complex with biologically molecules. In our previous studies we have proved that by engrafting amidine extremities as positively charged substituents at the end of the heteroaromatic substructures we could significantly improve the biological activity and orient the function of the molecule toward the binding to an electronegatively charged biological molecule such as DNA [1]. This work presents the synthesis of amidino substituted benzimidazoles and benzothiazoles as a potential biologically active agents. For the synthesis of novel targeted compounds classical organic synthesis reactions were used. Antitumor activity in 2D and 3D cancer cell culture assays on three human lung cancer cell lines (A549, HCC827, NCI-H358) was tested. Doxorubicin, staurosporine and vandetanib were used as control compounds [2].

amidines, benzimidazoles, benzothiazoles, antiproliferative activity

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