Hu, Caijuan; Li, Guoxun; Mu, Yu; Wu, Wenxi; Cao, Bixuan; Wang, Zixuan; Yu, Hainan; Guan, Peipei; Han, Li; Li, Liya; Huang, Xueshi published the artcile< Discovery of Anti-TNBC Agents Targeting PTP1B: Total Synthesis, Structure-Activity Relationship, In Vitro and In Vivo Investigations of Jamunones>, Name: 2,4,6-Trihydroxyisophthalaldehyde, the main research area is jamunone analog preparation antitumor triple neg breast cancer.
Twenty-three natural jamunone analogs 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 Me group on chromanone affected the selectivity of mols. against MDA-MB-231 and MCF-7 cells. Among them, jamunone M (I; JM) was screened as the most effective anti-triple-neg. 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.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 4396-13-8 belongs to class alcohols-buliding-blocks, and the molecular formula is C8H6O5, Name: 2,4,6-Trihydroxyisophthalaldehyde.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts