Disclosed are ((1R)-2-cyclopropyl-1-{ [(2S)-3-phenyl-2-(amino)propanoyl]amino} ethyl)boronic acid derivatives as represented by the general formula (I), or a pharmaceutically acceptable salt or boronic acid anhydride thereof, wherein: A is 0, 1, or 2； P is hydrogen, Rc-C(O)-, Rc-O-C(O)-, Rc-N(R4c)-C(O)-, Rc-S(O)2-, or Rc-N(R4c)-S(O)2-； Z1 and Z2 are each independently hydroxy, alkoxy, aryloxy, or aralkoxy； or Z1 and Z2 together form a moiety derived from a boronic acid complexing agent； and wherein the remaining substituents are as defined herein. Representative compounds include ((1R)-2-cyclopropyl-1-{ [(2S)-3-phenyl-2-({ [4-(pyridin-2-yloxy)phenyl]sulfonyl} amino)propanoyl]amino} ethyl)boronic acid, ((1R)-2-cyclopropyl-1-{ [(2S)-3-phenyl-2-({ [4-(pyridin-3-yloxy)phenyl]sulfonyl} amino)propanoyl]amino} ethyl)boronic acid, { (1R)-2-cyclopropyl-1-[((2S)-2-{ [(6-morpholin-4-ylpyridin-3-yl)sulfonyl]amino} -3-phenylpropanoyl)amino]ethyl} boronic acid, [(1R)-1-({ (2S)-2-[(1,3-benzothiazol-6-ylsulfonyl)amino]-3-phenylpropanoyl} amino)-2-cyclopropylethyl]boronic acid, ((1R)-2-cyclopropyl-1-{ [(2S)-2-({ [3-(2-methyl-1,3-thiazol-4-yl)phenyl]sulfonyl} amino)-3-phenylpropanoyl]amino} ethyl)boronic acid, { (1R)-2-cyclopropyl-1-[((2S)-2-{ [(1-methyl-1H-indol-4-yl)sulfonyl]amino} -3-phenylpropanoyl)amino]ethyl} boronic acid, [(1R)-2-cyclopropyl-1-({ (2S)-3-phenyl-2-[(pyrazin-2-ylcarbonyl)amino]propanoyl} amino)ethyl]boronic acid, ((1R)-2-cyclopropyl-1-{ [(2S)-3-phenyl-2-({ [4-(pyridin-3-ylsulfonyl)phenyl]sulfonyl} amino)propanoyl]amino} ethyl)boronic acid, ((1R)-1-{ [(2S)-2-({ [4-(1H-benzimidazol-5-yloxy)phenyl]sulfonyl} amino)-3-phenylpropanoyl]amino} -2-cyclopropylethyl)boronic acid and { (1R)-2-cyclopropyl-1-[((2S)-2-{ [(2-phenoxypyrimidin-5-yl)sulfonyl]amino} -3-phenylpropanoyl)amino]ethyl} boronic acid. Also disclosed is a pharmaceutical composition comprising a compound as defined above, and a pharmaceutically acceptable carrier or diluent, for use in treating cancer in a p
