《Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer》 was written by Wei, Mingming; Xie, Maodun; Zhang, Zhen; Wei, Yujiao; Zhang, Juan; Pan, Hongli; Li, Benlong; Wang, Jingjing; Song, Yang; Chong, Chuangke; Zhao, Rui; Wang, Jiefu; Yu, Li; Yang, Guang; Yang, Cheng. Computed Properties of C8H15BrO2 And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:
In this study, a class of novel HDACs inhibitors I (R = H, 4-CH3OC6H4; R1 = H, C6H5, 4-CH3OC6H4, 4-OHC6H4; R2 = H, OH; X = (CH2)n, n = 1, 3, 4, 5, 6, 7), II•HCl (R3 = N(CH3)2, 4-methylpiperazin-1-yl, morpholin-4-yl, piperidin-1-yl, pyrrolidin-1-yl; Y = (CH2)n, n = 5, 6, 7; Z = (CH2)n, n = 2, 3) was designed and synthesized based on the structure of flavones and isoflavones, followed by biol. evaluation. To be specific, a lead compound II•HCl [R3 = N(CH3)2; Y = (CH2)5; Z = (CH2)2 (III)] was discovered with strong anti-proliferative effects on a variety of solid tumor cells, especially for breast cancer cells with resistance to SAHA. Studies demonstrated that III could significantly inhibit the activity of HDAC 1,2,3 (class I) and 6 (class IIB), leading to a dose-dependent accumulation of acetylated histones and α-Tubulin, cell cycle arrest (G1/S phase) and apoptosis in breast cancer cells. Furthermore, the lead compound III could also antagonize the activation of STAT3 induced by HDACs inhibition in some breast cancer cells, which further reduced the level of pro-survive proteins in tumor cells and enhanced anti-tumor activity regulated by STAT3 signaling in vivo. Overall, findings demonstrated that the novel compound III might be a HDACs inhibitor candidate, which could be used as promising chemotherapeutic agent for breast cancer. The experimental part of the paper was very detailed, including the reaction process of 8-Bromooctanoic acid(cas: 17696-11-6Computed Properties of C8H15BrO2)
8-Bromooctanoic acid(cas: 17696-11-6) acid is used in the synthesis of 8-(N-Methyl-4,4′-bipyridinyl)- octanoic acid. 8-Mercaptooctanoic acid was prepared from 8-bromooctanoic acid. And 8-Bromooctanoic Acid is a useful compound for sonodynamic therapy.Computed Properties of C8H15BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary