Synthesis of Novel Phosphoramide-Tegafur Derivatives Containing Aminopropylsilatrane

Abstract

A series of novel phosphoramide-tegafur derivatives containing γ-aminopropyl silatrane were synthesized via the condensation reactions of phosphoryl dichloride with N¹-(2-furanidyl)-N³-(hydroxyethyl)-5-fluorouracil, followed by condensation with γ-aminopropyl silatrane. The structures of the products were confirmed by ¹H NMR, ³¹P NMR, IR, MS, and elemental analysis. The results of preliminary bioassay showed that the new compounds had an inhibition effect against HCT-8 and Bel-7402 cell lines.

Keywords:

• Anti-tumor activity
• γ-aminopropyl silatrane
• phosphoramide
• tegafur

We are grateful to the key project of the Chinese Ministry of Education‘(02140) and the dawn plan of science and technology for young scientists of Wuhan city (2002501024) for the financial support; we are also indebted to Prof. Guanhua Du who works at Beijing Institute of Medicine in Academy of Medical Sciences of China for antitumor activities test.