New discoveries in chemical research and development in 2021. The transformation of simple hydrocarbons into more complex and valuable products has revolutionised modern synthetic chemistry. In an article, author is El-Helby, Abdel-Ghany A., once mentioned the application of 120-21-8, Product Details of 120-21-8, Name is 4-Diethylaminobenzaldehyde, molecular formula is C11H15NO, molecular weight is 177.2429, category is benzoxazole. Now introduce a scientific discovery about this category.
Novel series of benzoxazoles 4(a-f)-16 were designed, synthesized, and evaluated for anticancer activity against HepG2, HCT-116, and MCF-7 cells. HCT-116 was the most sensitive cell line to the influence of the new derivatives. In particular, compound 5(e) was found to be the most potent against HepG2, HCT-116, and MCF-7 with IC50 = 4.13 +/- 0.2, 6.93 +/- 0.3, and 8.67 +/- 0.5 mu M, respectively. Compounds 5(c), 5(f), 6(b), 5(d), and 6(c) showed the highest anticancer activities against HepG2 cells with IC50 of 5.93 +/- 0.2, 6.58 +/- 0.4, 8.10 +/- 0.7, 8.75 +/- 0.7, and 9.95 +/- 0.9 mu M, respectively; HCT-116 cells with IC50 of 7.14 +/- 0.4, 9.10 +/- 0.8, 7.91 +/- 0.6, 9.52 +/- 0.5, and 12.48 +/- 1.1 mu M, respectively; and MCF-7 cells with IC50 of 8.93 +/- 0.6, 10.11 +/- 0.9, 12.31 +/- 1.0, 9.95 +/- 0.8, and 15.70 +/- 1.4 mu M, respectively, compared with sorafenib as a reference drug with IC50 of 9.18 +/- 0.6, 5.47 +/- 0.3, and 7.26 +/- 0.3 mu M, respectively. The most active compounds 5(c-f) and 6(b,c) were further evaluated for their vascular endothelial growth factor receptor-2 (VEGFR-2) inhibition. Compounds 5(e) and 5(c) potently inhibited VEGFR-2 at lower IC50 values of 0.07 +/- 0.01 and 0.08 +/- 0.01 mu M, respectively, compared with sorafenib (IC50 = 0.1 +/- 0.02 mu M). Compound 5(f) potently inhibited VEGFR-2 at low IC50 value (0.10 +/- 0.02 mu M) equipotent to sorafenib. Our design was based on the essential pharmacophoric features of the VEGFR-2 inhibitor sorafenib. Molecular docking was performed for all compounds to assess their binding pattern and affinity toward the VEGFR-2 active site.
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Reference:
Benzoxazole – Wikipedia,
,Benzoxazole | C7H5NO – PubChem