| 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. 17641247 - Inhibition of histone deacetylase activates side population cells in kidney and partial... |
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...