HPLC of Formula: C7H6O2. In 2019.0 BIOORG MED CHEM LETT published article about DEMETHYLASE 1 LSD1; ANTITUMOR-ACTIVITY; HISTONE; ANTIOXIDANT in [Wang, Jiming; Zhang, Xiangyu; Yan, Jiangkun; Li, Wei; Jiang, Qinwen; Wang, Xinran; Zhao, Dongmei; Cheng, Maosheng] Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, Shenyang 110016, Liaoning, Peoples R China in 2019.0, Cited 26.0. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4.
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.
HPLC of Formula: C7H6O2. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact Wang, JM; Zhang, XY; Yan, JK; Li, W; Jiang, QW; Wang, XR; Zhao, DM; Cheng, MS 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