Product Details of 25637-16-5In 2021 ,《Pyrazoloadenine Inhibitors of the RET Lung Cancer Oncoprotein Discovered by a Fragment Optimization Approach》 appeared in ChemMedChem. The author of the article were Saha, Debasmita; Ryan, Katie Rose; Lakkaniga, Naga Rajiv; Smith, Erica Lane; Frett, Brendan. The article conveys some information:
A fragment-based drug-discovery approach was used on a pyrazoloadenine fragment library to uncover new mols. that target the RET (REarranged during Transfection) oncoprotein, which is a driver oncoprotein in ∼2 % of non-small-cell lung cancers. The fragment library was screened against the RET kinase and LC-2/ad (RET-driven), KM-12 (TRKA-driven matched control) and A549 (cytotoxic control) cells to identify selective scaffolds that could inhibit RET-driven growth. An unsubstituted pyrazoloadenine fragment was found to be active on RET in a biochem. assay, but reduced cell viability in non-RET-driven cell lines (EC50=1 and 3 μM, resp.). To increase selectivity for RET, the pyrazoloadenine was modeled in the RET active site, and two domains were identified that were probed with pyrazoloadenine fragment derivatives to improve RET affinity. Scaffolds at each domain were merged to generate a novel lead compound, 8 p (I), which exhibited improved activity and selectivity for the RET oncoprotein (A549 EC50=5.92 μM, LC-2/ad EC50=0.016 μM, RET IC50=0.000326 μM). The experimental process involved the reaction of 4-Bromotetrahydropyran(cas: 25637-16-5Product Details of 25637-16-5)
4-Bromotetrahydropyran(cas: 25637-16-5) is often used as reactant for: preparation of anthranilic acids as antibacterial agents with human serum albumin binding affinity; preparation of antiatherogenic antioxidant di-tert-butyldihydrobenzofuranols via Grignard reactions with di-tert-butyl(hydroxy)benzaldehyde derivatives; synthesis of gephyrotoxin via the Schmidt reaction.Product Details of 25637-16-5
Referemce:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics