%0 Journal Article
%T Synthesis and antiretroviral evaluation of derivatives of zidovudine
%A Raviolo
%A M¨®nica A.
%A Trinchero-Hern¨¢ndez
%A Juan S.
%A Turk
%A Gabriela
%A Bri£¿¨®n
%A Margarita C.
%J Journal of the Brazilian Chemical Society
%D 2009
%I Sociedade Brasileira de Qu¨ªmica, SBQ
%R 10.1590/S0103-50532009001000015
%X a series of zidovudine (azt, 1) derivatives have been synthesized and their anti-hiv activity and cytotoxicity have been determined. the 5'-oh function of azt was derivatized using n, n'-carbonyldiimidazole and different amine compounds leading to their 5'-o-carbamates. in addition, two known azt derivatives 5'-o-tosylate and a tricyclic one (azt-cycl) were also obtained by a simpler procedure than those previously reported. although these azt derivatives were less toxic than azt, their reduced cytotoxicity was concomitant with an inability to inhibit hiv-1 replication, except in the case of azt-cycl, which showed an ic50 = 1 ¦̀mol l-1 without cytotoxicity with values of ccid50 ( ¦̀mol l-1) > 1000.
%K zidovudine analogs
%K anti-hiv activity
%K cytotoxicity.
%U http://www.scielo.br/scielo.php?script=sci_abstract&pid=S0103-50532009001000015&lng=en&nrm=iso&tlng=en