Authors Liu, G; Yin, T; Kim, Y; Ding, CY; Yu, Z; Wang, H; Chen, HY; Yan, RP; Wold, EA; Zou, H; Liu, X; Ding, Y; Shen, Q; Zhou, J in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about BIOLOGICAL EVALUATION; EXPRESSION; BCL-2; METASTASIS; APOPTOSIS; ANALOGS; GROWTH; TUMOR; CARBOPLATIN; COMBINATION in [Liu, Gang; Ding, Chunyong; Chen, Haiying; Wold, Eric A.; Ding, Ye; Zhou, Jia] Univ Texas Med Branch, Dept Pharmacol & Toxicol, Chem Biol Program, Galveston, TX 77555 USA; [Yin, Tao; Kim, Hyejin; Yu, Zhuo; Wang, Hong; Yan, Ruping; Zou, Hao; Liu, Xi; Shen, Qiang] Univ Texas MD Anderson Canc Ctr, Dept Clin Canc Prevent, Div Canc Prevent & Populat Sci, Houston, TX 77030 USA in 2019.0, Cited 44.0. Category: indole-building-block. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4
In an effort to develop novel Bax activators for breast cancer treatment, a series of diverse analogues have been designed and synthesized based on lead compound SMBA1 through several strategies, including introducing various alkylamino side chains to have a deeper access to S184 pocket, replacing carbon atoms with nitrogen, and reducing the nitro group of 9H-fluorene scaffold. Compounds 14 (CYD-2-11) and 49 (CYD-4-61) have been identified to exhibit significantly improved antiproliferative activity compared to SMBA1, with IC50 values of 3.22 mu M and 0.07 mu M against triple-negative breast cancer MDA-MB-231 and 3.81 mu M and 0.06 mu M against ER-positive breast cancer MCF-7 cell lines, respectively. Mechanism of action studies of compound 49 indicated that it can activate Bax protein to induce cytochrome c release and regulate apoptotic biomarkers, leading to cancer cell apoptosis. Further in vivo efficacy studies of compounds 14 and 49 in nude mice bearing MDA-MB-231 tumor xenografts demonstrated that these drug candidates can significantly suppress tumor growth, indicating their therapeutic potential for the treatment of breast cancer. (C) 2019 Elsevier Masson SAS. All rights reserved.
Welcome to talk about 100-83-4, If you have any questions, you can contact Liu, G; Yin, T; Kim, Y; Ding, CY; Yu, Z; Wang, H; Chen, HY; Yan, RP; Wold, EA; Zou, H; Liu, X; Ding, Y; Shen, Q; Zhou, J or send Email.. Category: indole-building-block
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