A Brief Review of the Anticancer Activity of α-Aminophosphonic Acid Derivatives and a Report on the in Vitro Activity of Some Dialkyl α-aryl- (or Heteroaryl)-α-(Diphenylmethylamino)Methanephosphonates

Abstract

Reports on the anticancer activity of representative α-aminophosphonic acid derivatives are briefly reviewed, with comments where possible on modes of action. Preliminary in vitro screening results are also presented for selected dialkyl α-aryl (or heteroaryl)-α-(diphenylmethylamino)methanephosphonates against the National Cancer Institute (NCI) 60-cell line panel of human tumor cells, which showed average response parameters for active compounds of GI₅₀ between 4.81 × 10⁻⁶ and 2.40 × 10⁻⁵ M, TGI between 1.88 and 6.28 × 10⁻⁵ M, and LC₅₀ between 5.71 and 9.37 × 10⁻⁵ M. The highest activity was shown by the α-phenyl compound for which GI₅₀ 10⁻⁷ M was recorded against leukemia cell line MOLT-4.

GRAPHICAL ABSTRACT

Keywords:

• Aminophosphonic acid
• aminophosphonate
• anticancer

ACKNOWLEDGMENTS

The authors thank the National Cancer Institute, National Institutes of Health, Bethesda, Maryland, USA, for anticancer screening and for the biological data reported in this paper. The authors are also grateful to Mr. John Crowder for the NMR measurements.