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Chem Commun (Camb). 2018 Jul 11;54(54):7479-7482. doi: 10.1039/c8cc04251a. Epub 2018 Jun 19.

Platination of cysteine by an epidermal growth factor receptor kinase-targeted hybrid agent.

Author information

1
Department of Chemistry, Wake Forest University, Wake Downtown Campus, Winston-Salem, NC 27101, USA. bierbau@wfu.edu.
2
Department of Internal Medicine, Section on Molecular Medicine, Wake Forest School of Medicine, Winston-Salem, NC 27157, USA.
3
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA.

Abstract

Hybrid molecules have been developed which are comprised of a tyrosine kinase-targeted, quinazoline-based scaffold and a flexibly linked dia(m)minechloridoPt(ii) moiety. The target compounds maintain high affinity and selectivity for ErbB family kinase proteins and one of the derivatives induces platinum adducts with a pharmacologically important cysteine residue.

PMID:
29915817
DOI:
10.1039/c8cc04251a
[Indexed for MEDLINE]

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