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Updated: Aug 17, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Efficient synthesis of fluorothiosparfosic acid analogues with potential antitumoral activity
Emmanuel Pfund1, Thierry Lequeux, Serge Masson
1Laboratoire de Chimie Moléculaire et Thio-organique (UMR CNRS 6507), ENSICAEN-Université de Caen, 6 Boulevard Maréchal Juin, F-14050 Caen, France.
Abstract:
In this paper, we describe a short synthesis of N-(phosphonoacetyl)-L-aspartate (PALA) analogues. The mono- and difluorinated thioacetamide precursors were prepared in one step from methyl (diethoxyphosphono)di- and monofluoromethyldithioacetates 8 and 11 as starting materials. Antiproliferating properties on a L1210 strain and ATCase inhibition of these new compounds are disclosed. ThioPALA(FF) 5c showed a remarkable cytotoxic activity towards murine leukemia L1210, when used as tetraester.
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