N1-substituted benzamidines: synthesis, antiproteinase activity and inhibition of tumor cell growth. |
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Authors: | R Ferroni D Simoni G Binato C Nastruzzi S Manfredini P Orlandini G Feriotto R Gambari |
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Affiliation: | Dipartimento di Scienze Farmaceutiche, Università di Ferrara. |
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Abstract: | We have synthesized N1-substituted benzamidines and poly-benzamidines with the aim to produce antitumor drugs retaining differential biological properties with respect to unsubstituted compounds. Antiproliferative activity on in vitro cultured human leukemic cells was exhibited by N1-substituted poly-benzamidines, while N1-substituted benzamidines were found to retain very low antitumor effects. Furthermore, our results suggest that N1-substituted benzamidines and some of poly-benzamidines exhibit low activity on trypsin and kallikrein. Taken together these data indicate that some N1-substituted poly-benzamidines could be of interest for experimental antitumor therapy, since are likely to retain low side effects due to alteration of proteinase activity. |
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