| 摘要 |
A compound of formula (I) or a pharmaceutically acceptable salt thereof: Preferably, the compound of formula (I) is 2-(bromoacetamido)phenylboronic acid. These compounds inhibit proteasome function in a mammal and as such, may be used to inhibit: the growth of a cell cancer, the rate of muscle protein degradation in a cell, activity of NF-kappa B, rate of intracellular protein breakdown, the rate of degradation of p53 protein in a cell, cyclin degradation in a cell, an inflammatory condition, antigen presentation in a cell, inducible NF-kappa B, HIV replication, and microbial infection in a patient. As such, the compounds of formula (I) are useful in the treatment of tissue rejection, organ rejection, arthritis, microbial infection, dermatoses, inflammatory bowel disease, asthma, osteoporosis, osteoarthritis, an autoimmune disease and cancer. In another aspect, a process for preparing 2-(bromoacetamido)phenylboronic acid by treating 2-aminophenylboronic acid pinacol ester with bromoacetylbromide followed by deprotection of the pinacol ester. |
