Document Detail

Synthesis and evaluation of isatin analogs as caspase-3 inhibitors: introduction of a hydrophilic group increases potency in a whole cell assay.
MedLine Citation:
PMID:  21441025     Owner:  NLM     Status:  MEDLINE    
A series of isatin analogs containing a hydrophilic group, including a pyridine ring, ethylene glycol group, and a triazole ring, have been synthesized, and their inhibition potency for caspase-3 was measured both in vitro (i.e., recombinant enzyme) and in whole cells (HeLa cells). The analogs having a hydrophilic group, including 12, 13, 16, 38, and 40, have dramatically increased activity in vitro and in HeLa cells compared to the corresponding unsubstituted N-phenyl isatin analogs.
Wenhua Chu; Justin Rothfuss; Dong Zhou; Robert H Mach
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural    
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  21     ISSN:  1464-3405     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2011 Apr 
Date Detail:
Created Date:  2011-04-04     Completed Date:  2011-07-19     Revised Date:  2014-09-21    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  2192-7     Citation Subset:  IM    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
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MeSH Terms
Caspase 3 / genetics,  metabolism
Caspase Inhibitors*
HeLa Cells
Hydrophobic and Hydrophilic Interactions
Isatin / analogs & derivatives*,  chemical synthesis,  pharmacology
Protease Inhibitors / chemical synthesis,  chemistry*,  pharmacology
Recombinant Proteins / chemistry,  genetics,  metabolism
Structure-Activity Relationship
Triazoles / chemistry
Grant Support
CA121952/CA/NCI NIH HHS; HL13851/HL/NHLBI NIH HHS; P01 HL013851/HL/NHLBI NIH HHS; P01 HL013851-42/HL/NHLBI NIH HHS; R21 CA121952/CA/NCI NIH HHS; R21 CA121952-01/CA/NCI NIH HHS; R21 CA121952-02/CA/NCI NIH HHS; R21 CA121952-03/CA/NCI NIH HHS; R21 CA121952-04/CA/NCI NIH HHS
Reg. No./Substance:
0/Caspase Inhibitors; 0/Protease Inhibitors; 0/Recombinant Proteins; 0/Triazoles; 82X95S7M06/Isatin; EC 3.4.22.-/Caspase 3

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