Issue 5, 2008
From the journal:

Organic & Biomolecular Chemistry

“Click” synthesis of small-molecule inhibitors targeting caspases†‡

Su Ling Ng,a   Peng-Yu Yang,ac   Kitty Y.-T. Chen,ac   Rajavel Srinivasana  and  Shao Q. Yao*abc  

* Corresponding authors

a Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore
E-mail: chmyaosq@nus.edu.sg
Fax: (+65) 67791691
Tel: (+65) 68741683

b Department of Biological Sciences, National University of Singapore, Singapore

c NUS MedChem Program of the Office of Life Sciences, National University of Singapore, Singapore

Abstract

A panel of 198 P4-diversified aldehyde (reversible) and vinyl sulfone (irreversible) inhibitors is successfully synthesized via an efficient “click chemistry” platform and directly screened against caspase-3 and -7 for inhibition.

Graphical abstract: “Click” synthesis of small-molecule inhibitors targeting caspases

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Article information

DOI
https://doi.org/10.1039/B718304F
Article type
Communication
Submitted
27 Nov 2007
Accepted
25 Jan 2008
First published
04 Feb 2008

Org. Biomol. Chem., 2008,6, 844-847

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“Click” synthesis of small-molecule inhibitors targeting caspases

S. L. Ng, P. Yang, K. Y.-T. Chen, R. Srinivasan and S. Q. Yao, Org. Biomol. Chem., 2008, 6, 844 DOI: 10.1039/B718304F

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