Recently I am researching about DEMETHYLASE 1 LSD1; ANTITUMOR-ACTIVITY; HISTONE; ANTIOXIDANT, Saw an article supported by the . Name: 3-Hydroxybenzaldehyde. Published in PERGAMON-ELSEVIER SCIENCE LTD in OXFORD ,Authors: Wang, JM; Zhang, XY; Yan, JK; Li, W; Jiang, QW; Wang, XR; Zhao, DM; Cheng, MS. The CAS is 100-83-4. Through research, I have a further understanding and discovery of 3-Hydroxybenzaldehyde
Histone lysine-specific demethylase 1 (LSD1) was the first discovered histone demethylase. Inactivating LSD1 or downregulating its expression inhibits cancer-cell development, and thus, it is an attractive molecular target for the development of novel cancer therapeutics. In this study, we worked on the structural optimization of natural products and identified 30 novel LSD1 inhibitors. Utilizing a structure-based drug design strategy, we designed and synthesized a series of curcumin analogues that were shown to be potent LSD1 inhibitors in the enzyme assay. Compound WB07 displayed the most potent LSD1 inhibitory activity, with an IC50 value of 0.8 mu M. Moreover, WA20 showed an anticlonogenic effect on A549 cells with an IC50 value of 4.4 mu M. Molecular docking simulations were also carried out, and the results indicated that the inhibitors bound to the protein active site located around the key residues of Asp555 and Asp556. These findings suggested that compounds WA20 and WB07 are the first curcumin analogue-based LSD1 inhibitors with remarkable A549 suppressive activity, providing a novel scaffold for the development of LSD1 inhibitors.
Name: 3-Hydroxybenzaldehyde. Bye, fridends, I hope you can learn more about C7H6O2, If you have any questions, you can browse other blog as well. See you lster.
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