Molecular Analysis of the Superior Efficacy of a Dual Epidermal Growth Factor Receptor (EGFR)-DNA-Targeting Combi-Molecule in Comparison with Its Putative Prodrugs 6-Mono-Alkylamino- and 6,6-Dialkylaminoquinazoline in a Human Osteosarcoma Xenograft Model

Molecular Analysis of the Superior Efficacy of a Dual Epidermal Growth Factor Receptor (EGFR)-DNA-Targeting Combi-Molecule in Comparison with Its Putative Prodrugs 6-Mono-Alkylamino- and 6,6-Dialkylaminoquinazoline in a Human Osteosarcoma Xenograft Model

<i>Background</i>: ZR2002 is a dual EGFR-DNA-targeting combi-molecule that carries a chloroethyl group at the six-position of the quinazoline ring designed to alkylate DNA. Despite its good pharmacokinetics, ZR2002 is metabolized in vivo into dechlorinated metabolites, losing the DNA-alk...

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Bibliographic Details
Main Authors: Caterina Facchin, Ana B. Fraga-Timiraos, Julie Schmitt, Nadia Babaa, Naveet Pannu, Antonio Aliaga, Anne-Laure Larroque, Bertrand J. Jean-Claude
Format: Article
Language:English
Published: MDPI AG 2023-03-01
Series:Cells
Subjects:
combi-molecule
osteosarcoma
DNA damage
EGFR
Online Access:https://www.mdpi.com/2073-4409/12/6/914

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