Issue 34, 2016
From the journal:

Chemical Communications

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

Hai-Jing Zhong,a   Bo Ra Lee,c   Joshua William Boyle,c   Wanhe Wang,b   Dik-Lung Ma,*b   Philip Wai Hong Chan*cd  and  Chung-Hang Leung*a  

* Corresponding authors

a State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao, China
E-mail: duncanleung@umac.mo

b Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China
E-mail: edmondma@hkbu.edu.hk

c School of Chemistry, Monash University, Clayton, Victoria 3800, Australia
E-mail: phil.chan@monash.edu

d Department of Chemistry, University of Warwick, Coventry, UK

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

DOI
https://doi.org/10.1039/C6CC01079B
Article type
Communication
Submitted
02 Feb 2016
Accepted
10 Mar 2016
First published
10 Mar 2016

Chem. Commun., 2016,52, 5788-5791

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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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