Artemisinin-polypyrrole conjugates: synthesis, DNA binding studies and preliminary antiproliferative evaluation. | - CCMAR -

Journal Article

TitleArtemisinin-polypyrrole conjugates: synthesis, DNA binding studies and preliminary antiproliferative evaluation.
Publication TypeJournal Article
AuthorsLa Pensée, L, Sabbani, S, Sharma, R, Bhamra, I, Shore, E, Chadwick, AE, Berry, NG, Firman, J, Araujo, NC, Cabral, LIL, Cristiano, MLS, Bateman, C, Janneh, O, Gavrila, A, Wu, YHang, Hussain, A, Ward, SA, Stocks, PA, Cosstick, R, O'Neill, PM
Year of Publication2013
JournalChemMedChem
Volume8
Issue5
Date Published2013 May
Pagination709-18
ISSN1860-7187
KeywordsAntineoplastic Combined Chemotherapy Protocols, Artemisinins, Binding Sites, Cell Proliferation, DNA, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, HL-60 Cells, HT29 Cells, Humans, Models, Molecular, Molecular Conformation, Molecular Dynamics Simulation, Parasitic Sensitivity Tests, Plasmodium falciparum, Polymers, Pyrroles, Structure-Activity Relationship, Thermodynamics
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.
DOI10.1002/cmdc.201200536
Sapientia

http://www.ncbi.nlm.nih.gov/pubmed/23495190?dopt=Abstract
Alternate JournalChemMedChem
PubMed ID23495190
CCMAR Authors
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