| 摘要 |
PCT No. PCT/GB93/01185 Sec. 371 Date Feb. 2, 1994 Sec. 102(e) Date Feb. 2, 1994 PCT Filed Jun. 3, 1993 PCT Pub. No. WO93/24475 PCT Pub. Date Dec. 9, 1993.Compounds of formula (1) are described wherein R represents a -CONHOH, carboxyl, carboxyl ester, or -P(O)(X1R8)X2R9, where X1 and X2 are the same or different and each is oxygen or sulphur, R8 and R9 are the same or different and each represents hydrogen or an optionally substituted alkyl, aryl or aralkylthioalkyl group; R2 represents an optionally substituted alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkoxy, or aralkylthio group, or an amino, substituted amino, carboxyl, or carboxyl ester group; R3 represents hydrogen or alkyl; R4 represents hydrogen or alkyl; R5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R7)- groups, where R7 is a hydrogen atom or a C1-6 alkyl group, or -(Alk)nR6 where Alk is an alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R7)- groups, n is zero or 1, and R6 is an optionally substituted cycloalkyl or cycloalkenyl group; X represents -NR10R11 where R10 is hydrogen or an optionally substituted alkyl, alkanoyl, aryl, aroyl, aralkyl or aralkanoyl group, and R11 is a straight or branched alkylaminosulphonylamino group wherein the alkyl portion is optionally interrupted by one or more -O- or -S- atoms of -N(R7)- or aminocarbonyloxy groups; or the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective inhibitory action against gelatinase and are useful in the treatment of cancer to control tumor metastasis.
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