Hu, Ming-Hao; Lin, Jia-Hong published the artcile< New Dibenzoquinoxalines Inhibit Triple-Negative Breast Cancer Growth by Dual Targeting of Topoisomerase 1 and the c-MYC G-Quadruplex>, SDS of cas: 27841-33-4, the main research area is dibenzoquinoxaline preparation breast cancer topoisomerase 1 MYC quadruplex inhibitor.
As c-MYC is one of the central players in triple-neg. breast cancer (TNBC) oncogenesis, inhibiting c-MYC expression would be an effective anticancer strategy. Transcription-induced neg. supercoiling is crucial in the regulation of c-MYC transcription, which facilitates the formation of a G4 structure in NHE III1 that can silence the transcription. However, topoisomerase 1 (Topo1) can dissipate this neg. supercoiling, leading to continuous activation of c-MYC transcription. Thus, dual ligands targeting both Topo1 and c-MYC G4 appear to be significant in cancer therapy. In this study, a series of new dibenzoquinoxaline derivatives were designed, synthesized, and evaluated for both Topo1 and c-MYC inhibition. Among them, 11-Methoxy-3,6-bis(4-methylpiperazin-1-yl)dibenzo[a,c]-phenazine was identified as the most promising dual ligand, which could effectively inhibit Topo1 activity and strongly stabilize c-MYC G4, thereby inhibiting cancer cell growth. Accordingly, this work suggests that this dual-targeting strategy may be effective in cancer therapy.
Journal of Medicinal Chemistry published new progress about Animal gene, c-myc Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 27841-33-4 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H12N2O2, SDS of cas: 27841-33-4.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics