Document Detail


Synthesis and biological activity of 7-phenyl-6,9-dihydro-3H-pyrrolo[3,2-f]quinolin-9-ones: a new class of antimitotic agents devoid of aromatase activity.
MedLine Citation:
PMID:  16539377     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The newly synthesized 7-phenyl-3H-pyrrolo[3,2-f]quinolinones 16-26 and previously 27 and 28 were assayed for their in vitro antiproliferative activity on tumor cell lines, and the lead compound 16 in vivo on a singenic hepatocellular carcinoma in Balb/c mice. Results from FACS, immunofluorescence microscopy analysis, tubulin polymerization assay, and tritiated water release assay for the CYP19 activity confirmed the new compounds as potential anticancer agents acting by tubulin depolymerization, but devoid of aromatase activity unlike their geometric [2,3-h] isomers.
Authors:
Venusia Gasparotto; Ignazio Castagliuolo; Gianfranco Chiarelotto; Vincenzo Pezzi; Daniela Montanaro; Paola Brun; Giorgio Palù; Giampietro Viola; Maria Grazia Ferlin
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  49     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2006 Mar 
Date Detail:
Created Date:  2006-03-16     Completed Date:  2006-04-28     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  1910-5     Citation Subset:  IM    
Affiliation:
Department of Pharmaceutical Sciences, University of Padova, 35131 Padova, Italy.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antimitotic Agents / chemical synthesis*,  chemistry,  pharmacology
Aromatase / metabolism*
Biopolymers
Cell Line, Tumor
Cell Proliferation / drug effects
Cytoskeleton / drug effects
Drug Screening Assays, Antitumor
Flow Cytometry
Humans
Mice
Microscopy, Fluorescence
Neoplasm Transplantation
Pyrroles / chemical synthesis*,  chemistry,  pharmacology
Quinolones / chemical synthesis*,  chemistry,  pharmacology
Structure-Activity Relationship
Transplantation, Isogeneic
Tritium
Tubulin / chemistry
Water / metabolism
Chemical
Reg. No./Substance:
0/7-phenyl-6,9-dihydro-3H-pyrrolo(3,2-f)quinolin-9-one; 0/Antimitotic Agents; 0/Biopolymers; 0/Pyrroles; 0/Quinolones; 0/Tubulin; 10028-17-8/Tritium; 7732-18-5/Water; EC 1.14.14.1/Aromatase

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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