Product Details of 89466-08-0In 2021 ,《Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogs as new KRASG12C inhibitors》 was published in European Journal of Medicinal Chemistry. The article was written by Xiao, Xuanzheng; Lai, Mengzhen; Song, Zilan; Geng, Meiyu; Ding, Jian; Xie, Hua; Zhang, Ao. The article contains the following contents:
KRAS is the most commonly altered oncogene of the RAS family, especially the G12C mutant (KRASG12C), which has been a promising drug target for many cancers. On the basis of the bicyclic pyridopyrimidinone framework of the first-in-class clin. KRASG12C inhibitor AMG510, a scaffold hopping strategy was conducted including a F-OH cyclization approach and a pyridinyl N-atom working approach leading to new tetracyclic and bicyclic analogs. Compound (I) was identified possessing binding potency of 1.87μM against KRASG12C and cell growth inhibition of 0.79μM in MIA PaCa-2 pancreatic cancer cells. Treatment of I with NCI-H358 cells resulted in down-regulation of KRAS-GTP levels and reduction of phosphorylation of downstream ERK and AKT dose-dependently. Mol. docking suggested that the fluorophenol moiety of I occupies a hydrophobic pocket region thus forming hydrogen bonding to Arg68. These results will be useful to guide further structural modification.2-Hydroxyphenylboronic acid(cas: 89466-08-0Product Details of 89466-08-0) was used in this study.
2-Hydroxyphenylboronic acid(cas: 89466-08-0) belongs to acyl phenylboronic acid. Phenylboronic acid (PBA), a synthetic molecule applied in RNA affinity chromatography, is able to form reversible covalent ester bonds with 1,2- or 1,3-cis-doils on the ribose ringProduct Details of 89466-08-0
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