Pavletic, Pegi; Semeano, Ana; Yano, Hideaki; Bonifazi, Alessandro; Giorgioni, Gianfabio; Piergentili, Alessandro; Quaglia, Wilma; Sabbieti, Maria Giovanna; Agas, Dimitrios; Santoni, Giorgio; Pallini, Roberto; Ricci-Vitiani, Lucia; Sabato, Emanuela; Vistoli, Giulio; Del Bello, Fabio published the artcile< Highly Potent and Selective Dopamine D4 Receptor Antagonists Potentially Useful for the Treatment of Glioblastoma>, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate, the main research area is glioblastoma antitumor D4R antagonists beta arrestin stem cells.
To better understand the role of dopamine D4 receptor (D4R) in glioblastoma (GBM), in the present paper, new ligands endowed with high affinity and selectivity for D4R were discovered starting from the brain penetrant and D4R selective lead compound 1-(3-(4-phenylpiperazin-1-yl)propyl)-3,4-dihydroquinolin-2(1H)-one (6). In particular, the D4R antagonist 24, showing the highest affinity and selectivity over D2R and D3R within the series (D2/D4 = 8318, D3/D4 = 3715), and the biased ligand 29, partially activating D4R Gi-/Go-protein and blocking β-arrestin recruitment, emerged as the most interesting compounds These compounds, evaluated for their GBM antitumor activity, induced a decreased viability of GBM cell lines and primary GBM stem cells (GSC#83), with the maximal efficacy being reached at a concentration of 10 μM. Interestingly, the treatment with both compounds 24 (I) and 29 (II) induced an increased effect in reducing the cell viability with respect to temozolomide, which is the first-choice chemotherapeutic drug in GBM.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Name: (9Z,12Z)-Methyl octadeca-9,12-dienoate.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics