Synthesis of half-mustard combi-molecules with fluorescence properties: correlation with EGFR status

Zakaria Rachid; Fouad Brahimi; Juozas Domarkas; Bertrand Jacques Jean-Claude

doi:10.1016/j.bmcl.2004.12.015

Synthesis of half-mustard combi-molecules with fluorescence properties: correlation with EGFR status

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1135-8. doi: 10.1016/j.bmcl.2004.12.015.

Authors

Zakaria Rachid¹, Fouad Brahimi, Juozas Domarkas, Bertrand Jacques Jean-Claude

Affiliation

¹ Cancer Drug Research Laboratory, Division of Medical Oncology, Department of Medicine, McGill University/Royal Victoria Hospital, 687 Pine Avenue west Rm M-719, Montreal, Québec, Canada H3A 1A1.

PMID: 15686928
DOI: 10.1016/j.bmcl.2004.12.015

Abstract

The synthesis of 6-(2-chloroethylamino)-4-anilinoquinazolines ZR2002 and ZR2003 designed to block EGFR tyrosine kinase and to damage genomic DNA is described. These compounds present fluorescence properties that permitted the quantitation of their subcellular uptake by flow cytometry. Fluorescence intensities increased with increasing levels of EGFR in a panel of isogenic and established cell lines.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antineoplastic Agents, Alkylating / chemical synthesis*
Antineoplastic Agents, Alkylating / chemistry
Antineoplastic Agents, Alkylating / pharmacology
Cell Line, Tumor
ErbB Receptors / antagonists & inhibitors*
ErbB Receptors / chemistry
Flow Cytometry
Fluorescence
Humans
Inhibitory Concentration 50
Neoplasm Proteins / antagonists & inhibitors
Nitrogen Mustard Compounds / chemical synthesis*
Nitrogen Mustard Compounds / chemistry
Nitrogen Mustard Compounds / pharmacology
Quinazolines / chemical synthesis*
Quinazolines / pharmacology
Structure-Activity Relationship

Substances

Antineoplastic Agents, Alkylating
Neoplasm Proteins
Nitrogen Mustard Compounds
Quinazolines
ErbB Receptors