engleski

Synthesis, cytostatic and antiviral activity of dialkyl 2-and 3-quinoline-substituted alpha-aminophosphonates

The chemistry and biochemistry of a-aminophosphonic acids and their derivatives have attracted current interest owing to their wide range of biological properties, with possible application from medicine to agriculture as enzyme inhibitors as well as antibacterial, anticancer and herbicidal agents. Recently, increasing attention has been devoted to nucleoside and nucleotide phosphonate analogues as broad-spectrum antiviral agents. Studying this class of phosphonic acid derivatives, we now report the synthesis, spectroscopic characterization and biological evaluation of novel dialkyl 2- and 3-quinoline-substituted a-aminophosphonates. As a preliminary assessment of their biological activity, complexes were evaluated for their in vitro cytostatic activity against human T-lymphoblast Molt4/C8 and CEM/0 cell lines and the murine leukemia L1210/0 tumor cell line, as well as for in vitro antiviral activity in different assay systems including a broad spectrum of DNA and RNA viruses. None of the examined compounds were found to exhibit cytostatic activity at therapeutically meaningful concentrations.

aminophosphonate; cytostatic activity; antiviral activity

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