Multitarget-Directed Drug Design Strategy:  A Novel Molecule Designed To Block Epidermal Growth Factor Receptor (EGFR) and To Exert Proapoptotic Effects

The multifactorial mechanistic nature of cancer calls for the development of multifunctional therapeutic tools, i.e., single compounds able to interact with multiple altered pathogenetic pathways. Following this rationale, we designed compounds able to irreversibly block epidermal growth factor rece...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2006-11, Vol.49 (23), p.6642-6645
Main Authors: Antonello, Alessandra, Tarozzi, Andrea, Morroni, Fabiana, Cavalli, Andrea, Rosini, Michela, Hrelia, Patrizia, Bolognesi, Maria Laura, Melchiorre, Carlo
Format: Article
Language:English
Subjects:
Aniline Compounds - chemical synthesis
Aniline Compounds - chemistry
Aniline Compounds - pharmacology
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Apoptosis
Biological and medical sciences
Cell Line, Tumor
Drug Design
Drug Screening Assays, Antitumor
General aspects
Humans
Medical sciences
Models, Molecular
Pharmacology. Drug treatments
Quinazolines - chemical synthesis
Quinazolines - chemistry
Quinazolines - pharmacology
Receptor, Epidermal Growth Factor - antagonists & inhibitors
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Summary:The multifactorial mechanistic nature of cancer calls for the development of multifunctional therapeutic tools, i.e., single compounds able to interact with multiple altered pathogenetic pathways. Following this rationale, we designed compounds able to irreversibly block epidermal growth factor receptor (EGFR), and to induce apoptosis in tumor cell lines. The novel molecules were synthesized by combining the structural features of the EGFR inhibitor PD153035 (1) and lipoic acid, which among other therapeutic effects triggers apoptosis in human cancer cells.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0608762