Artemisinin-Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation

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/m...

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Published inChemMedChem Vol. 8; no. 5; pp. 709 - 718
Main Authors La Pensée, Louise, Sabbani, Sunil, Sharma, Raman, Bhamra, Inder, Shore, Emma, Chadwick, Amy E., Berry, Neil G., Firman, James, Araujo, Nuna C., Cabral, Lília, Cristiano, Maria L. S., Bateman, Cerys, Janneh, Omar, Gavrila, Adelina, Wu, Yi Hang, Hussain, Afthab, Ward, Stephen A., Stocks, Paul A., Cosstick, Rick, O'Neill, Paul M.
Format Journal Article
LanguageEnglish
Published Weinheim WILEY-VCH Verlag 01.05.2013
WILEY‐VCH Verlag
Wiley
Wiley Subscription Services, Inc
Subjects
Antineoplastic Combined Chemotherapy Protocols - chemical synthesis
Antineoplastic Combined Chemotherapy Protocols - chemistry
Antineoplastic Combined Chemotherapy Protocols - pharmacology
artemisinin
Artemisinins - chemistry
Artemisinins - pharmacology
Binding Sites - drug effects
binding studies
Cell Proliferation - drug effects
Chemistry, Medicinal
cytotoxicity
DNA
DNA - chemistry
DNA - drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
HL-60 Cells
HT29 Cells
Humans
Life Sciences & Biomedicine
Models, Molecular
Molecular Conformation
Molecular Dynamics Simulation
molecular modelling
Parasitic Sensitivity Tests
Pharmacology & Pharmacy
Plasmodium falciparum - drug effects
Polymers - chemistry
Polymers - pharmacology
Pyrroles - chemistry
Pyrroles - pharmacology
Science & Technology
Structure-Activity Relationship
Thermodynamics
NETROPSIN
DRUG
LIGAND EFFICIENCY
molecular modelling
DOCKING
MALARIA PARASITES
GENETIC ALGORITHM
artemisinin
EFFICIENCY INDEXES
DNA
ANTIMALARIAL ACTIVITY
binding studies
DERIVATIVES
cytotoxicity
MINOR-GROOVE
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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.
AbstractList Greater than the sum of its parts: Artemisinins are currently in phaseI-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.
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.
Author Shore, Emma
Bateman, Cerys
Hussain, Afthab
Sabbani, Sunil
O'Neill, Paul M.
Bhamra, Inder
Cabral, Lília
Berry, Neil G.
Janneh, Omar
Stocks, Paul A.
Cristiano, Maria L. S.
Gavrila, Adelina
Sharma, Raman
La Pensée, Louise
Firman, James
Cosstick, Rick
Araujo, Nuna C.
Chadwick, Amy E.
Ward, Stephen A.
Wu, Yi Hang
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  surname: La Pensée
  fullname: La Pensée, Louise
  organization: Department of Chemistry, University of Liverpool, Crown Street, Liverpool, L69 7ZD (UK)
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  givenname: Sunil
  surname: Sabbani
  fullname: Sabbani, Sunil
  organization: Department of Chemistry, University of Liverpool, Crown Street, Liverpool, L69 7ZD (UK)
– sequence: 3
  givenname: Raman
  surname: Sharma
  fullname: Sharma, Raman
  organization: Department of Chemistry, University of Liverpool, Crown Street, Liverpool, L69 7ZD (UK)
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  givenname: Inder
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  fullname: Bhamra, Inder
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  givenname: Nuna C.
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  fullname: Araujo, Nuna C.
  organization: Centre of Marine Sciences (CCMAR), University of the Algarve, Campus de Gambelas, 8005-139, Faro (Portugal)
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Issue 5
Keywords NETROPSIN
DRUG
LIGAND EFFICIENCY
molecular modelling
DOCKING
MALARIA PARASITES
GENETIC ALGORITHM
artemisinin
EFFICIENCY INDEXES
DNA
ANTIMALARIAL ACTIVITY
binding studies
DERIVATIVES
cytotoxicity
MINOR-GROOVE
Language English
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SSID ssj0044818
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Snippet 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...
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...
Greater than the sum of its parts: Artemisinins are currently in phaseI-II clinical trials against breast, colorectal and non-small-cell lung cancers. In an...
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SubjectTerms Antineoplastic Combined Chemotherapy Protocols - chemical synthesis
Antineoplastic Combined Chemotherapy Protocols - chemistry
Antineoplastic Combined Chemotherapy Protocols - pharmacology
artemisinin
Artemisinins - chemistry
Artemisinins - pharmacology
Binding Sites - drug effects
binding studies
Cell Proliferation - drug effects
Chemistry, Medicinal
cytotoxicity
DNA
DNA - chemistry
DNA - drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
HL-60 Cells
HT29 Cells
Humans
Life Sciences & Biomedicine
Models, Molecular
Molecular Conformation
Molecular Dynamics Simulation
molecular modelling
Parasitic Sensitivity Tests
Pharmacology & Pharmacy
Plasmodium falciparum - drug effects
Polymers - chemistry
Polymers - pharmacology
Pyrroles - chemistry
Pyrroles - pharmacology
Science & Technology
Structure-Activity Relationship
Thermodynamics
Title Artemisinin-Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation
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https://onlinelibrary.wiley.com/doi/abs/10.1002%2Fcmdc.201200536
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https://www.ncbi.nlm.nih.gov/pubmed/23495190
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Volume 8
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