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Artemisinin-polypyrrole conjugates: synthesis, DNA binding studies and preliminary antiproliferative evaluation.
- Source :
-
ChemMedChem [ChemMedChem] 2013 May; Vol. 8 (5), pp. 709-18. Date of Electronic Publication: 2013 Mar 11. - Publication Year :
- 2013
-
Abstract
- Greater than the sum of its parts: Artemisinins are currently in phase I-II clinical trials against breast, colorectal and non-small-cell lung cancers. In an attempt to offer increased specificity, a series of hybrid artemisinin-polypyrrole minor groove binder conjugates are described. DNA binding/modelling studies and preliminary biological evaluation give insights into their mechanism of action and the potential of this strategy.<br /> (Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.)
- Subjects :
- Antineoplastic Combined Chemotherapy Protocols chemistry
Artemisinins chemistry
Binding Sites drug effects
Cell Proliferation drug effects
DNA chemistry
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
HL-60 Cells
HT29 Cells
Humans
Models, Molecular
Molecular Conformation
Molecular Dynamics Simulation
Parasitic Sensitivity Tests
Polymers chemistry
Pyrroles chemistry
Structure-Activity Relationship
Thermodynamics
Antineoplastic Combined Chemotherapy Protocols chemical synthesis
Antineoplastic Combined Chemotherapy Protocols pharmacology
Artemisinins pharmacology
DNA drug effects
Plasmodium falciparum drug effects
Polymers pharmacology
Pyrroles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1860-7187
- Volume :
- 8
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- ChemMedChem
- Publication Type :
- Academic Journal
- Accession number :
- 23495190
- Full Text :
- https://doi.org/10.1002/cmdc.201200536