NOVEL CHALCONE DERIVATIVES WITH CYTOTOXIC ACTIVITY

摘要

Chalcone derivatives of the general formula (I), wherein two from among A, B and Z which are adjacent to each other are linked and form a moiety selected from -O-(CH₂)_n-S(O)_m-, -S(O)_m-(CH₂)_n-O- and -O-(CH₂)_n-O-, and the remaining one from among A, B and Z is H; or two from among A, B and Z, independently from each other, are selected from a group consisting of OH, -O-C₁-C₆-alkyl and -S(O)m-C₁-C₆-alkyl, and the remaining one from among A, B and Z is H; R is H, C₁-C₆-alkyl, carboxy-C₁-C₆-alkyl, -(CH₂)_P- NR¹R² or O(CH₂)₃NH(CO)CF₃, where R¹ and R² both independently are C₁-C₆-alkyl; or R¹ and R² are linked together to form polymethylene group -(CH₂)_q-, and with N atom, to which they are attached, form a 5- or 6-membered ring, in which one of carbon atoms may be optionally replaced with O, N, or S; Y is -CH=CH-, -O-, -S- or -CH=N-; X¹, X², X³ independently are H, halogen atom, OH, -C₁-C₆-alkoxy, carboxy-C₁-C₆-alkoxyl, di(C₁-C₆- alkyl)amino-C₁-C₆-alkoxy, -0-PO(OH)₂, NO₂ or NH₂; m = O, 1 or 2; n = 1 or 2; p = 2 to 6; q = 4 or 5; and acid addition salts, salts with bases and C₁-C₆-alkyl esters thereof. The compounds may be useful as cytotoxic drugs for the treatment of neoplastic diseases. Formula (I).