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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 and Dove, Stefan and Sellmer, Andreas and Winkler, Matthias and Eichhorn, Emerich and Pongratz, Herwig and Ciossek, Thomas and Baer, Thomas and 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.

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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. ...

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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
Subjects: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
Owner: Prof. Dr. Stefan Dove
Deposited On:10 Jul 2009 06:25
Last Modified:05 Aug 2009 13:58
Item ID:8551
Owner Only: item control page
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