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    
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.
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 :
8607847 - Aggregation of the inactive form of human alpha-galactosidase in the endoplasmic reticu...
18166657 - Real-time imaging reveals that noninvasive mammary epithelial acini can contain motile ...
25284987 - Phyllostachys edulis extract induces apoptosis signaling in osteosarcoma cells, associa...
18601077 - Rheological characteristics of cell suspension and cell culture of perilla frutescens.
11559557 - Alpha2,6-sialylation of cell-surface n-glycans inhibits glioma formation in vivo.
22541327 - Effect of post-fusion holding time, orientation and position of somatic cell-cytoplasts...
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.
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

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...