An article Design, synthesis and biological evaluation of novel pteridinone derivatives as potent dual inhibitors of PLK1 and BRD4 WOS:000575065200022 published article about BROMODOMAIN; CANCER in [Qi, Yinliang; Xu, Le; Li, Zhiwei; Gong, Ping; Qin, Mingze; Liu, Yajing; Zhao, Yanfang; Hou, Yunlei] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, 103 Wenhua Rd, Shenyang 110016, Peoples R China; [Hu, Tao; Yin, Bixi; Hou, Yunlei] Yangtze River Pharmaceut Grp Co Ltd, 1 South Yangtze River Rd, Taizhou 225321, Peoples R China in 2020.0, Cited 19.0. The Name is 1,1,1-Triethoxyethane. Through research, I have a further understanding and discovery of 78-39-7. SDS of cas: 78-39-7
To develop novel simultaneous inhibition of PLK1 and BRD4 bromodomain by a single molecule, three series of novel pteridinone derivatives were designed, synthesized and evaluated for their biological activity. Most compounds exhibited moderate to excellent cytotoxic activity against A549, HCT116, PC-3 and MCF-7 cell lines. The most promising compoundIII(4)showed high antiproliferative effects on four cell lines with IC(50)values of 1.27 mu M, 1.36 mu M, 3.85 mu M and 4.06 mu M, respectively. The enzymatic assay identifiedIII(4)as a potent PLK1 and BRD4 dual inhibitor with % inhibition values of 96.6 and 59.1, respectively. Furthermore, to clarify the anticancer mechanism of the target compounds, explorations in the bioactivity were conducted. The results showed that compoundIII(4)obviously inhibited the proliferation of HCT-116 cell lines, induced a great decrease in the mitochondrial membrane potential leading to apoptosis of cancer cells, suppressed the migration of tumor cells, and arrested the S phase of HCT116 cells.
SDS of cas: 78-39-7. Bye, fridends, I hope you can learn more about C8H18O3, If you have any questions, you can browse other blog as well. See you lster.
Reference:
Thiazolidine – Wikipedia,
,Thiazolidine – ScienceDirect.com