Safety of 4-Methoxybenzaldehyde. Authors Mohamed, AR; El Kerdawy, AM; George, RF; Georgey, HH; Gawad, NMA in ACADEMIC PRESS INC ELSEVIER SCIENCE published article about in [Mohamed, Abdalla R.] Egyptian Russian Univ, Dept Pharmaceut Chem, Fac Pharm, Cairo 11829, Egypt; [Kerdawy, Ahmed M. El; George, Riham F.; Georgey, Hanan H.; Gawad, Nagwa M. Abdel] Cairo Univ, Dept Pharmaceut Chem, Fac Pharm, Cairo 11562, Egypt; [Kerdawy, Ahmed M. El] New Giza Univ, Dept Pharmaceut Chem, Fac Pharm, Km 22 Cairo Alexandria Desert Rd, Cairo, Egypt; [Georgey, Hanan H.] Heliopolis Univ Sustainable Dev, Dept Pharmaceut Chem, Fac Pharm, Cairo 11777, Egypt in 2021, Cited 90. The Name is 4-Methoxybenzaldehyde. Through research, I have a further understanding and discovery of 123-11-5
Aiming to obtain an efficient anti-proliferative activity, structure- and ligand-based drug design approaches were expanded and utilized to design and refine a small compound library. Subsequently, thirty-two 7,8-disubstituted-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione derivatives were selected for synthesis based on the characteristic pharmacophoric features required for PI3K and B-Raf oncogenes inhibition. All the synthesized compounds were evaluated for their in vitro anticancer activity. Compounds 17 and 22c displayed an acceptable potent activity according to the DTP-NCI and were further evaluated in the NCI five doses assay. To validate our design, compounds with the highest mean growth inhibition percent were screened against the target PI3K alpha and B-Raf(V)(600E) to confirm their multi-kinase activity. The tested compounds showed promising multi-kinase activity. Compounds 17 and 22c anticancer effectiveness and multi-kinase activity against PI3K alpha and B-Raf(V)(600E) were consolidated by the inhibition of B-Raf(WT), EGFR and VEGFR-2 with IC50 in the sub-micromolar range. Further investigations on the most potent compounds 17 and 22c were carried out by studying their safety on normal cell line, in silico profiling and predicted ADME characteristics.
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Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles