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• W2097698114 startingPage "1163" @default.
• W2097698114 abstract "We have previously reported the synthesis of SMA41, a unimolecular combination of an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) of the quinazoline class and a DNA-damaging monomethyltriazene termed “combimolecule”. Hydrolysis of 1-[4-(<i>m</i>-tolylamino)-6-quinazolinyl]-3-methyltriazene (SMA41) gives rise to an intact TKI [6-amino-4-(3-methylanilino)quinazoline; SMA52] capable of inhibiting epidermal growth factor (EGF)-induced EGFR autophosphorylation and a DNA-targeting methyldiazonium species. Herein, we showed that SMA41 blocked EGF-induced EGFR autophosphorylation by an irreversible mechanism, suggesting that it may covalently damage the receptor in these cells. More importantly, this was associated with significant inhibition of mitogen-activated protein kinase activation in A431 cells. In cells treated with [¹⁴C]SMA41, radio-high-performance liquid chromatography detection of both <i>N</i>⁷- and <i>O</i>⁶-methylguanine revealed an almost complete repair of the <i>O</i>⁶-methylguanine lesions and a greater tolerance of the <i>N</i>⁷-methylguanine adducts 24 h post-treatment. In contrast to temozolomide (a cyclic triazene used in the clinic) and the reversible inhibitor SMA52, SMA41 induced significant cell cycle arrest in S, G2, and M phases 24 h after a 2-h drug exposure. Furthermore, in vivo studies demonstrated that SMA41 was well tolerated. At 200 mg/kg, it showed approximately 2-fold greater antiproliferative activity than SMA52 in A431 cells implanted in immunocompromised SCID mice. These results suggest that the binary targeting properties of SMA41 are associated with a binary cascade of events in the cells that seem to culminate into significant growth inhibition in vitro and in vivo." @default.
• W2097698114 created "2016-06-24" @default.
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• W2097698114 date "2004-09-09" @default.
• W2097698114 modified "2023-10-18" @default.
• W2097698114 title "The Combi-Targeting Concept: Dissection of the Binary Mechanism of Action of the Combi-Triazene SMA41 in Vitro and Antitumor Activity in Vivo" @default.
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• W2097698114 doi "https://doi.org/10.1124/jpet.104.071977" @default.
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