4463-02-9Relevant articles and documents
A Nouvel Route to Resorcinols
Gesson, Jean-Pierre,Jacquesy, Jean-Claude,Jouannetaud, Marie-Paule
, p. 1128 - 1129 (1980)
Hydroxylation of para-alkylated or 2,6-dialkylated phenols by hydrogen peroxide in SbF5-HF yields resorcinols, the electrophile reacting with the O-protonated substrate.
HALOGEN-SUBSTITUTED DIMETHYLCHALCONE DERIVATIVES AND PREPARATION METHOD THEREOF
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, (2021/04/13)
The present invention relates to dimethylchalcone (DMC) derivatives substituted with halogen and a method for producing the same. A compound according to an embodiment of the present invention is represented by chemical formula I: [Chemical Formula I]. In Formula I, R1 and R2 are the same as or different from each other, R1, and R2 are each independently selected from the group consisting of hydrogen, methoxy, and methoxy. R3, and R4 are each independently hydrogen or halogen elements, and when R3 is hydrogen, R4 R4 is any one selected from the group consisting of halogen elements R3.
Discovery of Anti-TNBC Agents Targeting PTP1B: Total Synthesis, Structure-Activity Relationship, in Vitro and in Vivo Investigations of Jamunones
Hu, Caijuan,Li, Guoxun,Mu, Yu,Wu, Wenxi,Cao, Bixuan,Wang, Zixuan,Yu, Hainan,Guan, Peipei,Han, Li,Li, Liya,Huang, Xueshi
, p. 6008 - 6020 (2021/05/06)
Twenty-three natural jamunone analogues along with a series of jamunone-based derivatives were synthesized and evaluated for their inhibitory effects against breast cancer (BC) MDA-MB-231 and MCF-7 cells. The preliminary structure-activity relationship revealed that the length of aliphatic side chain and free phenolic hydroxyl group at the scaffold played a vital role in anti-BC activities and the methyl group on chromanone affected the selectivity of molecules against MDA-MB-231 and MCF-7 cells. Among them, jamunone M (JM) was screened as the most effective anti-triple-negative breast cancer (anti-TNBC) candidate with a high selectivity against BC cells over normal human cells. Mechanistic investigations indicated that JM could induce mitochondria-mediated apoptosis and cause G0/G1 phase arrest in BC cells. Furthermore, JM significantly restrained tumor growth in MDA-MB-231 xenograft mice without apparent toxicity. Interestingly, JM could downregulate phosphatidylinositide 3-kinase (PI3K)/Akt pathway by suppressing protein-tyrosine phosphatase 1B (PTP1B) expression. These findings revealed the potential of JM as an appealing therapeutic drug candidate for TNBC.