Recently I am researching about EPITHELIAL-MESENCHYMAL TRANSITION; ANTICONVULSANT ACTIVITIES; BIOLOGICAL EVALUATION; CANCER; ANTIBACTERIAL; PROLIFERATION; INHIBITION; APOPTOSIS; POTENT, Saw an article supported by the National Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [81960626, 82060628]; Doctoral Research Startup Foundation of Yanbian University [602020087]. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Shang, FF; Wang, JY; Xu, Q; Deng, H; Guo, HY; Jin, XJ; Li, XT; Shen, QK; Quan, ZS. The CAS is 123-11-5. Through research, I have a further understanding and discovery of 4-Methoxybenzaldehyde. Computed Properties of C8H8O2
Four series of hypoxia-inducible factor-1 alpha (HIF-1 alpha) functioning derivatives stemming from modifications to the C-29 carboxyl group of celastrol were designed and synthesized, and their anticancer activities were evaluated. To address the structure and activity relationship of each derivative, extensive structural changes were made. HRE luciferase reporter assay demonstrated that 12 modified compounds showed superior HIF-1 alpha inhibitory activity. Among them, compound C6 exhibited the best features: firstly, the strongest HIF-1 alpha inhibitory activity (IC50 = 0.05 mu M, 5-fold higher than that of celastrol); secondly, lower cytotoxicity (22-fold lower, C6-16.85 mu M vs celastrol-0.76 mu M). Thus, the safety factor of C6 was about 112 times higher than that of celastrol. Western blot assay indicated that C6 may inhibit the expression of HIF-1 alpha protein in cells. Additionally, C6 hindered tumor cell cloning, migration and induced cell apoptosis. It is worth mentioning that in the mouse tumor xenograft model, C6 (10 mg/kg) displayed good antitumor activity in vivo, showing a better inhibition rate (74.03%) than the reference compound 5-fluorouracil (inhibition rate, 59.58%). However, the celastrol treatment group experienced collective death after four doses of the drug. Moreover, C6 minimally affected the mouse weight, indicating that its application in vivo has little toxic effect. H&E staining experiments show that it could also exacerbate the degree of tumor cell damage. The results of water solubility experiment show that the solubility of C6 is increased by 1.36 times than that of celastrol. In conclusion, C6 is a promising antitumor agent through HIF-1 alpha pathway. (C) 2021 Elsevier Masson SAS. All rights reserved.
Computed Properties of C8H8O2. About 4-Methoxybenzaldehyde, If you have any questions, you can contact Shang, FF; Wang, JY; Xu, Q; Deng, H; Guo, HY; Jin, XJ; Li, XT; Shen, QK; Quan, ZS or concate me.
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