| Identification of the Spiro(oxindole-3,3'-thiazolidine)-Based Derivatives as Potential p53 Activity Modulators. | |
| | |
MedLine Citation:
|
PMID: 21058726 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
|
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. |
| | |
Authors:
|
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 |
Related Documents
:
|
10557106 - The cellular response to p53: the decision between life and death. 8622896 - Abrogation of wild-type p53 mediated growth-inhibition by nuclear exclusion. 18059176 - Ciprofloxacin-induced g2 arrest and apoptosis in tk6 lymphoblastoid cells is not depend... 14751676 - Foetal rat lung epithelial (frle) cells: alterations in cellular homeostasis and gene e... 19960406 - Insulin-like growth factor binding protein-3 induces g1 cell cycle arrest with inhibiti... 11991756 - Rep/cap gene amplification and high-yield production of aav in an a549 cell line expres... |
Publication Detail:
|
Type: JOURNAL ARTICLE Date: 2010-11-8 |
Journal Detail:
|
Title: Journal of medicinal chemistry Volume: - ISSN: 1520-4804 ISO Abbreviation: - Publication Date: 2010 Nov |
Date Detail:
|
Created Date: 2010-11-9 Completed Date: - Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: - |
Other Details:
|
Languages: ENG Pagination: - Citation Subset: - |
Affiliation:
|
Department of Pharmaceutical and Toxicological Chemistry, University of Naples "Federico II", Italy. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: In Vitro Synthesis of Betaxanthins Using Recombinant DOPA 4,5-Dioxygenase and Evaluation of Their Ra...
Next Document: Scytonemides A and B, cyclic peptides with 20S proteasome inhibitory activity from the cultured cyan...