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The synthesis of analogs of the lactacystin-derived beta-lactone (2) in whi
ch the substituents at C(5), C(7) and C(9) were systematically varied has l
ed to a well defined structure-activity correlation for the highly selectiv
e inhibition of the mammalian 20 S proteasome. (C) 1999 Elsevier Science Lt
d. All rights reserved.