摘要：New thia.olo[4,5-d]pyrimidines 4a. b, thioxopropa.oic a.id ethyl ester 7 a.d 4-oxothia.olidine benzenesulfona.ides 9a.h were designed a.d synthesized. The molecula. design wa. performed using MOE (Molecula. Opera.ing Environment) softwa.e to predict the binding mode of the proposed compounds on hCa.II. a.l the newly synthesized compounds were eva.ua.ed for their in-vitro a.tica.cer a.tivity a.a.nst liver ca.cer cell line (HEPG-2) in which hCa.I is overexpressed. The a.tivity of the screened compounds wa. compa.ed with tha. of doxorubicin, the reference drug. The ra.iosensitizing a.ility of the promising compounds 3, 4b, 9b wa. studied which showed a. increa.e in the cell killing effect of γ-ra.ia.ion a.ter combina.ion with them.