Abstract
A new series of 1,3-oxazole attached to bromonabumetone derivatives have been
designed and in silico studying as molecular docking using (GOLD) suite program and determination of pharmacokinetic properties using Swiss ADME suite,
and then best fitting compounds were synthesized successfully, and
confirmed using spectral analysis FT-IR, 1 HNMR and 13 CNMR. In vitro evaluation as an anti-proliferative activity for epidermal growth factor receptor (EGFR)
Tyrosine kinase using MTT assay. The anti-proliferative investigation revealed a
dose-dependent impact on lung cancer cells (A549) with inhibitory concentration
IC50 for compounds 4b and 4c (6.14 & 14.8) µM, respectively which was significantly higher than that of erlotininb IC50 = 24.6 µM. While compound 4a had
IC50 (26.8) µM, which is closely related to erlotininb.
Keywords: 1,3-Oxazole, EGFR, nabumetone, A549 cell line, molecular docking,
pharmacokinetic study
Subject
Infectious Diseases,Applied Microbiology and Biotechnology,Epidemiology,Biotechnology
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