Synthesis and Biological Evaluation of Novel Phosphonates Derivatives of As Potential Antitumor Agents

Abstract

A series of dialkyl [2-(4,6-dimethoxypyrimidin-2-yloxy)benzamido](aryl) methylphosphonates derivatives were designed and synthesized. All the new compounds were identified by elemental analysis, IR, ¹H NMR, ³¹P NMR, and MS. Their antitumor activity against KB and CNE1 cells was examined. Some of the compounds showed potential antitumor activity, which provided some hints for further study of structure modification. In particular, the compounds 6i and 6j displayed more potent cytotoxic activities against KB in comparison with 5-FU.

[Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements for the following free supplemental resource: Table S1]

GRAPHICAL ABSTRACT

Keywords:

• Phosphonate
• pyrimidinylbenzoate
• amide
• antitumor activity