Identification of new shikonin derivatives as STAT3 inhibitors was written by Qiu, Han-Yue;Fu, Jiang-Yan;Yang, Min-Kai;Han, Hong-Wei;Wang, Peng-Fei;Zhang, Ya-Han;Lin, Hong-Yan;Tang, Cheng-Yi;Qi, Jin-Liang;Yang, Rong-Wu;Wang, Xiao-Ming;Zhu, Hai-Liang;Yang, Yong-Hua. And the article was included in Biochemical Pharmacology (Amsterdam, Netherlands) in 2017.Safety of Ethyl 2-(4-fluorophenyl)acetate This article mentions the following:
The signal transducer and activator of transcription 3 is a constitutively activated oncogenic protein in various human tumors and represents a valid target for anticancer drug design. In this study, the authors have achieved a new type of STAT3 inhibitors based on structural modifications on shikonin scaffold, guided by computational modeling. By tests, PMMB-187 exhibited a more outstanding profile than shikonin on a small panel of human breast cancer cells, especially for the MDA-MB-231 cells. For the cellular mechanisms research, PMMB-187 was found to induce cell apoptosis in MDA-MB-231 cells, associated with the reduction of mitochondrial membrane potential, production of ROS and alteration of the levels of apoptosis-related proteins. Furthermore, PMMB-187 inhibited constitutive/inducible STAT3 activation, transcriptional activity, nuclear translocation and downstream target genes expression in STAT3-dependent breast cancer cells MDA-MB-231. Besides, no obvious inhibitory effect on activation of STAT1 and STAT5 was observed with PMMB-187 treatment. Most notably, the in vivo studies further revealed that PMMB-187 could dramatically suppress the MDA-MB-231 cells xenografted tumor growth. The in vitro and in vivo results collectively suggest that PMMB-187 may serve as a promising lead compound for the further development of potential therapeutic anti-neoplastic agents. In the experiment, the researchers used many compounds, for example, Ethyl 2-(4-fluorophenyl)acetate (cas: 587-88-2Safety of Ethyl 2-(4-fluorophenyl)acetate).
Ethyl 2-(4-fluorophenyl)acetate (cas: 587-88-2) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Safety of Ethyl 2-(4-fluorophenyl)acetate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics