84212-46-4Relevant articles and documents
Synthesis of Novel Vindoline-Chrysin Hybrids
Mayer, Szabolcs,Nagy, Nóra,Keglevich, Péter,Szigetvári, áron,Dékány, Miklós,Szántay Junior, Csaba,Hazai, László
, (2021/12/09)
Vinca alkaloids are well-known microtubule targeting agents, which are used against some types of cancer. Vindoline is one of the monomeric Vinca alkaloids which does not have anti-tumor effect, although its derivatives have serious impact on the field of
Design and synthesis of novel Flavone-based histone deacetylase inhibitors antagonizing activation of STAT3 in breast cancer
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
, (2020/08/21)
Histone deacetylases (HDACs) inhibitors have demonstrated a great clinical achievement in hematological malignancies. However, the efficacy of HDACs inhibitors in treating solid tumors remains limited due to the complicated tumor microenvironment. In this study, we designed and synthesized a class of novel HDACs inhibitors based on the structure of flavones and isoflavones, followed by biological evaluation. To be specific, a lead compound 15a 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 15a 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 15a 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, our findings demonstrated that the novel compound 15a might be a HDACs inhibitor candidate, which could be used as promising chemotherapeutic agent for breast cancer.
Flavonoid compound and application thereof to anti-cancer medicine
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Paragraph 0039; 0042; 0043; 0044, (2018/07/30)
The invention provides a flavonoid compound and application thereof to an anti-cancer medicine. The compound is of a structure of formula (I) shown in the specification, wherein m is 1 to 10; R1 and R2 are respectively selected from hydrogen, hydroxyl, and unsubstituted aryl and heteroaryl or aryl and heteroaryl which are substituted by one or more first substituent groups; X is selected from hydrogen, hydroxyl, nitryl, halogen, amino or cyano; R3 is selected from hydrogen, hydroxyl and -O(CH2)nN(R4R5); n is 2 to 10; R4 and R5 are respectively selected from hydrogen, unsubstituted C1-C10 alkylor C1-C10 alkyl which is substituted by one or more second substituent groups, C2-C12 alkenyl, C1-C10 halogenated alkyl, C2-C12 halogenated alkenyl, C2-C14 heteroalkyl, C2-C12 alkeneoxy, C1-C6 alkyneoxy, amino, C1-C10 alkyl amino, C1-C10 amino alkyl, C1-C10 alkyl carbonyl, C1-C10 carbalkoxy, C1-C10 alkyl amino carbonyl, C1-C10 alkyl carbonyl or C5-C12 aryl carbonyl.
