abstract |
Disclosed are depsipeptides of formulae (I) and (I'), wherein R1-R4 are amino acid side chain moieties, each R6 is the same or different and represents hydrogen or C1-C4 alkyl; and Pr1 and Pr2 are the same or different and represent hydrogen or a thiol-protecting group; or a pharmaceutically acceptable salt thereof. The compounds are FK228 analogues useful in the treatment of diseases mediated by HDAC such as cancer, cardiac hypertrophy, chronic heart failure, inflammatory conditions, cardiovascular diseases, haemoglobinopathy, thalassemia, sickle cell disease, CNS disorders, autoimmune diseases, diabetes, osteoporosis, MDS, benign prostatic hyperplasia, oral leukoplakia, genetically related metabolic disorders, infections, Rubens-Taybi, fragile X syndrome, or alpha-1 antitrypsin deficiency, for accelerating wound healing, or as an immunosuppressant. |