Document Detail

Identification of the Spiro(oxindole-3,3'-thiazolidine)-Based Derivatives as Potential p53 Activity Modulators.
MedLine Citation:
PMID:  21058726     Owner:  NLM     Status:  In-Data-Review    
Here, we report the design of new analogues of spirooxoindolepyrrolidine nucleus as modulators of p53 activity. Compounds (3R,7aR)-6-(4-chlorobenzyl)-1H-spiro[imidazo[1,5-c]thiazole-3,3'-indoline]-2',5,7(6H,7aH)-trione (9c) and (3R,7aR)-5'-methyl-6-(3,4,5-trimethoxybenzyl)-1H-spiro[imidazo[1,5-c]thiazole-3,3'-indoline]-2',5,7(6H,7aH)-trione (10d) are the most potent compounds of this series, inhibiting cell growth of different human tumor cells at submicromolar and micromolar concentrations, respectively. Compound 9c induces apoptotic cell death in human melanoma cell line M14 at 24 h, while in the same condition, treatment with 10d showes a clear arrest at G2/M phase inducing delay of cell cycle progression. Possibly, these activities may be due to inhibition of p53-MDM2 interaction and subsequent p53 release and activation.
Isabel Gomez-Monterrey; Alessia Bertamino; Amalia Porta; Alfonso Carotenuto; Simona Musella; Claudio Aquino; Ilaria Granata; Marina Sala; Diego Brancaccio; Delia Picone; Carmine Ercole; Paola Stiuso; Pietro Campiglia; Paolo Grieco; Pio Ianelli; Bruno Maresca; Ettore Novellino
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Publication Detail:
Type:  Journal Article     Date:  2010-11-08
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  53     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2014-02-04     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  8319-29     Citation Subset:  IM    
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