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Easy Derivatisation of Group 10 N‐Heterocyclic Carbene Complexes and In Vitro Evaluation of an Anticancer Oestradiol Conjugate
Author(s) -
Chardon Edith,
Puleo Gian Luigi,
Dahm Georges,
Fournel Sylvie,
Guichard Gilles,
BelleminLaponnaz Stéphane
Publication year - 2012
Publication title -
chempluschem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.801
H-Index - 61
ISSN - 2192-6506
DOI - 10.1002/cplu.201200092
Subject(s) - carbene , conjugate , chemistry , combinatorial chemistry , solubility , metal , in vitro , polyethylene glycol , palladium , ruthenium , organic chemistry , stereochemistry , catalysis , biochemistry , mathematical analysis , mathematics
In the search for novel metal‐based pharmaceuticals, ruthenium‐catalysed 1,3‐dipolar cycloaddition is used to functionalise a series of palladium and platinum N‐heterocyclic carbene complexes. This strategy was applied to the conjugation of amino acid, polyethylene glycol and oestradiol derivatives with the aim of enhancing chemical diversity and introducing specific features (e.g., water solubility, cell targeting). Antiproliferative activities of the different complexes were assayed against several cancer cell lines (KB, MCF7, HCT116, PC3, SKOV3, OVCAR8, HL60) and healthy cell lines (MRC5, VERO, EPC), which established their efficiency. The ease of the structural derivatisation thus renders these complexes attractive metal‐based systems for the development of selective targeted metal‐hybrid anticancer drugs.