| 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 |
Related Documents
:
|
20472437 - Synthesis and antitumor activity of 2,5-bis(3'-indolyl)-furans and 3,5-bis(3'-indolyl)-... 19023807 - Apoptotic cell death through inhibition of protein kinase ckii activity by 3,4-dihydrox... 10935497 - Novel suicide ligands of tubulin arrest cancer cells in s-phase. 21544357 - Efficient adenovirus-mediated gene transfer into human cancer cell lines derived from d... 14751527 - Predicting response to treatment in human cancers of the uterine cervix: sequential bio... 19936817 - Glutamine as indispensable nutrient in oncology: experimental and clinical evidence. |
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. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| 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
Previous Document: A systematic study of C-glucoside trisphosphates as myo-inositol trisphosphate receptor ligands. Syn...
Next Document: Spatial conformation and topography of the tyrosine aromatic ring in substrate recognition by protei...