Small-Molecule Kinase-Inhibitors-Loaded Boron Cluster as Hybrid Agents for Glioma-Cell-Targeting Therapy

Marcos Couto; Ignacio Mastandrea; Mauricio Cabrera; Pablo Cabral; Francesc Teixidor; Hugo Cerecetto; Clara Viñas

doi:10.1002/chem.201701965

Small-Molecule Kinase-Inhibitors-Loaded Boron Cluster as Hybrid Agents for Glioma-Cell-Targeting Therapy

Marcos Couto, Ignacio Mastandrea, Mauricio Cabrera, Pablo Cabral, Francesc Teixidor, Hugo Cerecetto^*, Clara Viñas

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

Abstract

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.

Original language	English
Pages (from-to)	9233-9238
Number of pages	6
Journal	Chemistry - A European Journal
Volume	23
Issue number	39
DOIs	https://doi.org/10.1002/chem.201701965
State	Published - 12 Jul 2017
Externally published	Yes

Keywords

carboranes
cross-coupling
cycloaddition
glioblastoma multiforme
synthetic methods

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1002/chem.201701965

Cite this

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abstract = "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{\textquoteright} 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.",

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AU - Couto, Marcos

AU - Mastandrea, Ignacio

AU - Cabrera, Mauricio

AU - Cabral, Pablo

AU - Teixidor, Francesc

AU - Cerecetto, Hugo

AU - Viñas, Clara

PY - 2017/7/12

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N2 - 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.

AB - 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.

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KW - glioblastoma multiforme

KW - synthetic methods

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Small-Molecule Kinase-Inhibitors-Loaded Boron Cluster as Hybrid Agents for Glioma-Cell-Targeting Therapy

Abstract

Keywords

UN SDGs

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