Go to content
UR Home

Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases.

Mahboobi, Siavosh, Dove, Stefan, Sellmer, Andreas, Winkler, Matthias, Eichhorn, Emerich, Pongratz, Herwig, Ciossek, Thomas, Baer, Thomas, Maier, Thomas and Beckers, Thomas (2009) Design of chimeric histone deacetylase- and tyrosine kinase-inhibitors: a series of imatinib hybrides as potent inhibitors of wild-type and mutant BCR-ABL, PDGF-Rbeta, and histone deacetylases. Journal of medicinal chemistry 52 (8), pp. 2265-79.

Full text not available from this repository.

at PubMed

at publisher (via DOI)


Abstract

Inhibitors of histone deacetylases are a new class of cancer therapeutics with possibly broad applicability. Combinations of HDAC inhibitors with the kinase inhibitor 1 (Imatinib) in recent studies showed additive and synergistic effects. Here we present a new concept by combining inhibition of protein kinases and HDACs, two independent pharmacological activities, in one synthetic small molecule. ...

plus


Export bibliographical data



Item type:Article
Date:2009
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz)
Identification Number:
ValueType
19301902PubMed ID
10.1021/jm800988rDOI
Classification:
NotationType
AcetylationMESH
Benzamides/chemical synthesisMESH
Cell Line, TumorMESH
Cell Proliferation/drug effectsMESH
Drug Screening Assays, AntitumorMESH
Histone Deacetylases/antagonists & inhibitorsMESH
Histones/metabolismMESH
HumansMESH
Models, MolecularMESH
MutationMESH
Phthalic Acids/chemical synthesisMESH
Piperazines/chemical synthesisMESH
Protein-Tyrosine Kinases/antagonists & inhibitorsMESH
Pyrimidines/chemical synthesisMESH
Receptor, Platelet-Derived Growth Factor beta/antagonists & inhibitorsMESH
StereoisomerismMESH
Structure-Activity RelationshipMESH
Thiazoles/chemical synthesisMESH
Thiophenes/chemical synthesisMESH
Dewey Decimal Classification:500 Science > 570 Life sciences
500 Science > 540 Chemistry & allied sciences
600 Technology > 610 Medical sciences Medicine
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Partially
Item ID:8551
Owner only: item control page
  1. Homepage UR

University Library

Publication Server

Contact:

Publishing: oa@ur.de

Dissertations: dissertationen@ur.de

Research data: daten@ur.de

Contact persons