Document Detail


Dimeric 3,5-bis(benzylidene)-4-piperidones: A novel cluster of tumour-selective cytotoxins possessing multidrug-resistant properties.
MedLine Citation:
PMID:  22409967     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
A series of bis[3,5-bis(benzylidene)-4-oxo-1-piperidinyl]amides 1 display potent cytotoxic properties towards a wide range of tumours. A number of the CC(50) and IC(50) values are in the range of 10(-8) M. Specifically, these compounds have the following important properties. First, greater toxicity was demonstrated towards certain tumours than various non-malignant cells. Second, various compounds in series 1 are toxic to a number of human colon cancer and leukaemic cells. Third, these compounds reverse P-gp mediated multidrug resistance. Various prototypic molecules such as 1a,b and 1i were identified as lead molecules for further studies. A representative lead molecule 1b induces apoptosis via internucleosomal DNA fragmentation and PARP cleavage in HSC-2 and HL-60 cells while flow cytometry revealed that this compound blocked the G2/M and S-phases in the cell cycle of human colon cancer HCT-116 cells.
Authors:
Swagatika Das; Umashankar Das; Hiroshi Sakagami; Naoki Umemura; Shoko Iwamoto; Tomohiko Matsuta; Masami Kawase; Joseph Molnár; Julianna Serly; Dennis K J Gorecki; Jonathan R Dimmock
Related Documents :
22767597 - Aurora b is regulated by the mitogen-activated protein kinase/extracellular signal-regu...
22447567 - Mre11-dependent degradation of stalled dna replication forks is prevented by brca2 and ...
8607847 - Aggregation of the inactive form of human alpha-galactosidase in the endoplasmic reticu...
8076527 - Inhibition of urokinase synthesis and cell surface binding alters the motile behavior o...
22272057 - Mixed type of malignant mesothelioma in an aged male icr mouse.
23719257 - Mechanical models for the self-organization of tubular patterns.
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-2-27
Journal Detail:
Title:  European journal of medicinal chemistry     Volume:  -     ISSN:  1768-3254     ISO Abbreviation:  -     Publication Date:  2012 Feb 
Date Detail:
Created Date:  2012-3-13     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0420510     Medline TA:  Eur J Med Chem     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Affiliation:
Drug Design and Discovery Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, 110 Science Place, Saskatoon, Saskatchewan S7N 5C9, Canada.
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:  Is local ointment or cauterization more effective in childhood recurrent epistaxis.
Next Document:  Synthesis of new troglitazone derivatives: Anti-proliferative activity in breast cancer cell lines a...