Syntheses and Antitumor Activities of Purine-sulfonamides Derivatives†

Abstract

As a new type of purine derivative,Roscovitine exhibits good antiproliferative activities to different types of tumor cell lines and currently has been investigated in Phase Ⅱ clinical trial. Previous structure-activity relationship studies on Roscovitine suggested that the modification on C2,C6 and N9 positions of purine could significantly influence the antitumor acitivities. In this work,a biologically active fragment benzenesulfonamide was introduced to purine C2 position and totally 25 new purine-sulfonamides derivatives were synthesized and evaluated antiproliferative activities in some tumor cell lines by MTT assay. The results show that the substitutions on C2,N6 and N9 positions of purine have a great impact on antitumor activity. And introducing phenylsulfonyl piperazine on C2 position of purine could obviously enhance antiproliferative activities. Among them,compound 17d shows similar inhibitory activities against PC-3,HCT116 and K562 tumor cell lines compared with Roscovitine.