Document Detail

Synthesis of selenophene derivatives as novel CHK1 inhibitors.
MedLine Citation:
PMID:  20674356     Owner:  NLM     Status:  MEDLINE    
A series of selenophene derivatives 3 were synthesized as potential CHK1 inhibitors. The effects of substitution on the 4'- or 5'-position of selenophene moiety and shifting the hydroxyl group position on C6- phenolic ring of oxindole were explored. This study led to the discovery of the most potent CHK1 inhibitors 29-33 and 39-43, which had IC(50) values in the subnanomolar range.
Pao-Chiung Hong; Li-Jung Chen; Tzu-Yun Lai; Huei-Yu Yang; Shih-Jan Chiang; Yann-Yu Lu; Ping-Kuei Tsai; Hung-Yi Hsu; Win-Yin Wei; Chu-Bin Liao
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-07-13
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  20     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2010 Sep 
Date Detail:
Created Date:  2010-08-16     Completed Date:  2010-12-06     Revised Date:  2011-11-02    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  5065-8     Citation Subset:  IM    
Copyright Information:
Copyright 2010 Elsevier Ltd. All rights reserved.
Development Center for Biotechnology, Xizhi City, Taipei County, Taiwan.
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MeSH Terms
Protein Kinase Inhibitors / chemical synthesis*,  pharmacology
Protein Kinases / drug effects*
Selenium Compounds / chemical synthesis*,  pharmacology
Reg. No./Substance:
0/Protein Kinase Inhibitors; 0/Selenium Compounds; EC 2.7.-/Protein Kinases; EC kinase 1

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