| 摘要 |
The invention relates to new peptidyl derivatives, with the formula I: <IMAGE> in which R represents a -CONHOH, carboxyl (-CO2H) or esterified carboxyl group; R1 represents an alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group, which may possibly be substituted; R2 represents an alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkoxy, or aralkylthio group, which may possibly be substituted, or an amino (-NH), substituted amino, carboxyl (-CO2H) or esterified carboxyl group; R3 represents a hydrogen atom or an alkyl group; R4 represents a hydrogen atom or an alkyl group; R5 represents an -[Alk]nR6 group, in which Alk represents an alkyl or alkenyl group which may possibly be interrupted by one or more -O- or -S- atoms or -N(R7)- groups [in which R7 represents a hydrogen atom or an alkyl group with 1 to 6 carbon atoms], n is 0 or a whole number 1, and R6 represents a cycloalkyl or cycloalkenyl group, which may be substituted; X represents an amino (-NH2), substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and have in particular a selective action against gelatinases, and can be used in the treatment of cancer in order to control the development of metastases of the tumour.
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