The present invention is directed to 5-substituted thio-camptothecinderivatives of the formula (l)(see formula I)wherein:R is hydrogen or -N3;R1 is hydrogen, ethyl or the group ¨CH=N-O-C(CH3)3;R2 is hydrogen or ¨CH2N(CH3)2;R3 is hydrogen or the group (see formula II) ; andpharmaceutically acceptable salts, isomers, enantiomers, diastereomersthereof and mixtures thereof having antitumor activity, the processes for thepreparation thereof, the use thereof as antitumor drugs and pharmaceuticalcompositions containing them.