摘要：New thi.zolo[4,5-d]pyri.i.i.es 4a, b, thi.xopropanoi. aci. ethyl ester 7 and 4-oxothi.zoli.i.e benzenesulfonami.es 9a-h were desi.ned and synthesi.ed. The molecular desi.n was performed usi.g MOE (Molecular Operati.g Envi.onment) software to predi.t the bi.di.g mode of the proposed compounds on hCA i.. All the newly synthesi.ed compounds were evaluated for thei. i.-vi.ro anti.ancer acti.i.y agai.st li.er cancer cell li.e (HEPG-2) i. whi.h hCAi. i. overexpressed. The acti.i.y of the screened compounds was compared wi.h that of doxorubi.i., the reference drug. The radi.sensi.i.i.g abi.i.y of the promi.i.g compounds 3, 4b, 9b was studi.d whi.h showed an i.crease i. the cell ki.li.g effect of γ-radi.ti.n after combi.ati.n wi.h them.