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Artemisinin–Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation
Author(s) -
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.
Publication year - 2013
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201200536
Subject(s) - artemisinin , computer science , polypyrrole , computational biology , minor groove , conjugate , chemistry , dna , nanotechnology , medicine , biology , biochemistry , polymerization , materials science , immunology , mathematics , mathematical analysis , plasmodium falciparum , organic chemistry , malaria , polymer
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.