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Small‐Molecule Kinase‐Inhibitors‐Loaded Boron Cluster as Hybrid Agents for Glioma‐Cell‐Targeting Therapy
Author(s) -
Couto Marcos,
Mastandrea Ignacio,
Cabrera Mauricio,
Cabral Pablo,
Teixidor Francesc,
Cerecetto Hugo,
Viñas Clara
Publication year - 2017
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201701965
Subject(s) - glioma , erlotinib , cancer research , lipophilicity , cytotoxic t cell , epidermal growth factor receptor , targeted therapy , cancer cell , chemistry , cytotoxicity , in vitro , cancer , biology , biochemistry , receptor , genetics
The reported new anilinoquinazoline‐icosahedral borane hybrids have been evaluated as glioma targeting for potential use in cancer therapy. Their anti ‐glioma activity depends on hybrids’ lipophilicity; the most powerful compound against glioma cells, a 1,7‐ closo ‐derivative, displayed at least 3.3 times higher activity than the parent drug erlotinib. According to the cytotoxic effects on normal glia cells, the hybrids were selective for epidermal growth factor receptor (EGFR)‐overexpressed tumor cells. These boron carriers could be used to enrich glioma cancer cells with boron for cancer therapy.