Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors |
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Authors: | Liu Lee Tai Yuan Ta-Tung Liu Hung-Huang Chen Shyh-Fong Wu Ying-Ta |
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Affiliation: | Development Center for Biotechnology, 102 Lane 169 Kang Ning Street, Xi Zhi, Taipei, Taiwan, ROC. letliu@yahoo.com.tw |
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Abstract: | A series of C-6 or C-3' alkynyl-substituted 4-anilinoquinazoline derivatives was prepared straightforwardly by a Sonogashira reaction of the corresponding bromo-substituted 4-anilinoquinazolines. Bioactive assay of these compounds for in vitro EGFR kinase inhibition demonstrated that the novel 6-hydroxypropynyl-4-anilinoquinazoline 5e was a very potent EGFR kinase inhibitor with an IC(50) of 14 nM. |
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