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Issue 34, 2016
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Structure-based screening and optimization of cytisine derivatives as inhibitors of the menin–MLL interaction

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Abstract

The natural product-like compound 1 was identified as a direct inhibitor of the menin–MLL interaction by in silico screening. Structure-based optimization furnished analogue 1a, which showed significantly higher potency than both the lead structure 1 and the reference compound MI-2.

Graphical abstract: Structure-based screening and optimization of cytisine derivatives as inhibitors of the menin–MLL interaction

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Article information


Submitted
02 Feb 2016
Accepted
10 Mar 2016
First published
10 Mar 2016

Chem. Commun., 2016,52, 5788-5791
Article type
Communication

Structure-based screening and optimization of cytisine derivatives as inhibitors of the menin–MLL interaction

H. Zhong, B. R. Lee, J. W. Boyle, W. Wang, D. Ma, P. W. Hong Chan and C. Leung, Chem. Commun., 2016, 52, 5788
DOI: 10.1039/C6CC01079B

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