Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 23, Pages 6642-6645Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm0608762
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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.
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