Jiang, Jie published the artcileA2B Adenosine Receptor Antagonists with Picomolar Potency, Synthetic Route of 67914-60-7, the publication is Journal of Medicinal Chemistry (2019), 62(8), 4032-4055, database is CAplus and MEDLINE.
The A2B adenosine receptor (A2BAR) was proposed as a novel target for the (immuno)therapy of cancer since A2BAR blockade results in antiproliferative, anti-angiogenic, anti-metastatic, and immuno-stimulatory effects. In this study, we explored the structure-activity relationships of xanthin-8-yl-benzenesulfonamides mainly by introducing a variety of linkers and substituents attached to the sulfonamide residue. A new, convergent strategy was established which facilitated the synthesis of the target compounds Many of the new compounds exhibited subnanomolar affinity for the A2BAR combined with high selectivity. Functional groups were introduced which will allow the attachment of dyes and other reporter groups. 8-(4-((4-(4-Bromophenyl)piperazin-1-yl)sulfonyl)phenyl)-1-propylxanthine (34, PSB-1901) was the most potent A2B-antagonist (Ki 0.0835 nM, KB 0.0598 nM, human A2BAR) with >10,000-fold selectivity vs. all other AR subtypes. It was similarly potent and selective at the mouse A2BAR, making it a promising tool for preclin. studies. Computational studies predicted halogen bonding to contribute to the outstanding potency of 34.
Journal of Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Synthetic Route of 67914-60-7.
Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics