C. Meier et al., CYCLIC SALIGENYL PHOSPHOTRIESTERS OF 2',3'-DIDEOXY-2',3'-DIDEHYDROTHYMIDINE (D4T) - A NEW PRO-NUCLEOTIDE APPROACH, Bioorganic & medicinal chemistry letters, 7(2), 1997, pp. 99-104
The synthesis of a new pro-nucleotide approach for d4TMP 2 based on cy
cloSal-d4TMP 3a-d is described. Phosphotriesters 3 release d4TMP 2 sel
ectively by a controlled, chemically induced tandem reaction. CycloSal
-phosphotriesters 3 exhibited high biological activity against HIV-1/H
IV-2 in CEM cells which was retained in CEM TK- cells. (C) 1997, Publi
shed by Elsevier Science Ltd.