the design and synthesis of a new class of rtk/hdac dual-targeted inhibitors

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ID: 228476
2013
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Abstract
Over the years, the development of targeted medicines has made significant achievements. As a typical example, receptor tyrosine kinases (RTK) inhibitors have become important chemotherapy drugs for a variety of cancers. However, the effectiveness of these agents is always hindered by poor response rates and acquired drug resistance. In order to overcome these limitations, several dual-targeted inhibitors with quinazoline core were designed and synthesized. Though these compounds can simultaneously inhibit histone deacetylases (HDAC) as well as RTK, the structure-activity relationship (SAR) is still not clear enough. To further explore this type of dual-targeted inhibitors, a new class of quinazoline derivatives were designed and synthesized. Their activity evaluations include in vitro inhibitory activity of HDAC, epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). The SAR study indicated that the introduction of polar group such as hydroxamate on the 4-position of the quinazoline core is more likely to provide a potent HDACi/HER2i hybrid rather than HDACi/EGFRi molecule.
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lu2013moleculesthe Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;Wei Lu;Jia Li;Xuan Zhang;Yi Chen;Mingbo Su
Journal Journal of ethnopharmacology
Year 2013
DOI
10.3390/molecules18066491
URL
http://www.mdpi.com/1420-3049/18/6/6491
Keywords
synergistic effect antitumor receptor tyrosine kinases histone deacetylase

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