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Synfacts 2011(7): 0704-0704  
DOI: 10.1055/s-0030-1260479
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of MLN4924

Contributor(s): Philip Kocienski
H. W. Lee, S. K. Nam, W. J. Choi, H. O. Kim, L. S. Jeong*
Ewha Womans University, Seoul and Dongguk University, Kyungki-do, Korea
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Publication History

Publication Date:
17 June 2011 (online)

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Significance

MLN4924 is an adenosine monophosphate mimic that inhibits the NEDD8 activating enzyme resulting in S-phase defects, DNA damage, and apoptosis. It is currently in phase I clinical trials for the treatment of various cancers. The enantiospecific synthesis depicted is based on a chiral pool strategy that begins with d-ribose.