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• W2546093669 abstract "Dual inhibition of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER-2) is an attractive cancer therapeutic approach. In this study, new series of 4-anilinothieno[2,3-d]pyrimidines were designed, synthesized, and tested as dual EGFR/HER-2 kinase inhibitors. Five compounds (8a, 8b, 8e-g) demonstrated low to submicromolar inhibition of both kinases with IC50 values of 1.2, 0.6, 0.3, 0.2, 0.4 μM and 8.2, 3.4, 1.3, 0.5, 2.7 μM for the EGFR and HER-2, respectively. Introduction of a 5,6-tetramethylene moiety into the thienopyrimidine core bearing a 4-(3-fluorobenzyloxy)-3-chloroaniline tail resulted in a favorable increase in both the EGFR and HER-2 inhibitory activities. Compound 8f (IC50 EGFR/HER-2: 0.2/0.5 μM) also exhibited significant cell growth inhibition on some specific NCI cell lines, especially ovarian, breast, non-small-cell lung cancer, and renal cancer cell lines." @default.
• W2546093669 created "2016-11-04" @default.
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• W2546093669 date "2016-10-13" @default.
• W2546093669 modified "2023-10-10" @default.
• W2546093669 title "Design and Synthesis of 4-Anilinothieno[2,3-<i>d</i> ]pyrimidine-Based Compounds as Dual EGFR/HER-2 Inhibitors" @default.
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• W2546093669 doi "https://doi.org/10.1002/ardp.201600197" @default.
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