Format

Send to

Choose Destination
J Enzyme Inhib Med Chem. 2014 Jun;29(3):338-43. doi: 10.3109/14756366.2013.782024. Epub 2013 Apr 11.

Design, synthesis and evaluation of 2-phenylisothiazolidin-3-one-1,1-dioxides as a new class of human protein kinase CK2 inhibitors.

Author information

1
Institute of Molecular Biology and Genetics, NAS of Ukraine , Kyiv , Ukraine and.

Abstract

The synthesis and in vitro evaluation of 40 new 2-phenylisothiazolidin-3-one-1,1-dioxide derivatives are described. The optimization based on biological screening data and molecular modeling resulted in a 10-fold increase in inhibitory activity compared with previously reported inhibitors of this class and led to the identification of 3-{[2-chloro-4-(1,1-dioxido-3-oxoisothiazolidin-2-yl)benzoyl]amino}benzoic acid, a potent inhibitor of human protein kinase CK2 (ІC₅₀ = 1.5 μM).

KEYWORDS:

2-phenylisothiazolidin-3-one-1,1-dioxides; CK2 inhibitors; molecular docking

PMID:
23578312
DOI:
10.3109/14756366.2013.782024
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Taylor & Francis
Loading ...
Support Center