Synthesis, Identification, and Structure-Activity Relationship Analysis of GATA4 and NKX2-5 Protein-Protein Interaction Modulators was written by Jumppanen, Mikael;Kinnunen, Sini M.;Valimaki, Mika J.;Talman, Virpi;Auno, Samuli;Bruun, Tanja;Boije af Gennas, Gustav;Xhaard, Henri;Aumuller, Ingo B.;Ruskoaho, Heikki;Yli-Kauhaluoma, Jari. And the article was included in Journal of Medicinal Chemistry in 2019.Reference of 54802-10-7 This article mentions the following:
Transcription factors GATA4 and NKX2-5 directly interact and synergistically activate several cardiac genes and stretch-induced cardiomyocyte hypertrophy. Previously, we identified phenylisoxazole carboxamide 1 as a hit compound, which inhibited the GATA4-NKX2-5 transcriptional synergy. Here, the chem. space around the mol. structure of 1 was explored by synthesizing and characterizing 220 derivatives and structurally related compounds In addition to the synergistic transcriptional activation, selected compounds were evaluated for their effects on transcriptional activities of GATA4 and NKX2-5 individually as well as potential cytotoxicity. The structure-activity relationship (SAR) anal. revealed that the aromatic isoxazole substituent in the southern part regulates the inhibition of GATA4-NKX2-5 transcriptional synergy. Moreover, inhibition of GATA4 transcriptional activity correlated with the reduced cell viability. In summary, comprehensive SAR anal. accompanied by data anal. successfully identified potent and selective inhibitors of GATA4-NKX2-5 transcriptional synergy and revealed structural features important for it. In the experiment, the researchers used many compounds, for example, 3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7Reference of 54802-10-7).
3-Aminobenzofuran-2-carboxamide (cas: 54802-10-7) belongs to benzofurans derivatives. Benzofurans are only weakly aromatic in nature and they are cleaved by many oxidative and reductive conditions. Benzofurans are stable towards alkali and readily polymerize on treatment with sulfuric acid, due to which they are useful for the preparation of low cost chemically relatively inert resins.Reference of 54802-10-7
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem