{"id":10276,"date":"2022-10-20T01:52:11","date_gmt":"2022-10-19T17:52:11","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10276"},"modified":"2022-10-20T01:52:11","modified_gmt":"2022-10-19T17:52:11","slug":"ran-kais-team-published-research-in-european-journal-of-medicinal-chemistry-in-2021-08-05-1046832-21-6","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10276","title":{"rendered":"Ran, Kai’s team published research in European Journal of Medicinal Chemistry in 2021-08-05 | 1046832-21-6"},"content":{"rendered":"

Ran, Kai; Zeng, Jun; Wan, Guoquan; He, Xiaojie; Feng, Zhanzhan; Xiang, Wang; Wei, Wei; Hu, Xiang; Wang, Ningyu; Liu, Zhihao; Yu, Luoting published the artcile< Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors>, Application of C11H19BN2O2<\/a>, the main research area is pyridopyrimidinone preparation antitumor activity FGFR inhibitor; FGFR; Solubility; Tumor growth inhibition; pyrido[1,2-a]pyrimidinone.<\/p>\n

Herein, the design and synthesis of pyrido[1,2-a]pyrimidinone derivatives I (R1 = methoxyethoxy, tert-butoxycarbonyl-1,2,3,6-tetrahydropyridin-4-yl, 1H-pyrazol-4-yl, etc.) and II (R2 = Me, azetidin-3-yl, etc.; R3 = 3-[(propan-2-yl)amino]propyl, prop-2-yn-1-yl, cyclopropylmethyl, etc.) as potent FGFR inhibitors were described. Examination of structure-activity relationships and preliminary assessment identified I (R1 = 1-methyl-1H-pyrazol-4-yl) as a novel FGFR inhibitor that displayed excellent potency in vitro. Candidate I [R1 = 1-methyl-1H-pyrazol-4-yl (III)] suppressed the phosphorylation of FGFR signaling pathways and induced cell cycle arrest and apoptosis at low nanomolar concentration In the kinase inhibition profile, III showed excellent kinase selectivity for the FGFR family. Furthermore, III showed higher aqueous solubility than Erdafitinib. Moreover, III exhibited potent antitumor activity (tumor growth inhibition = 106.4%) in FGFR2-amplified SNU-16 gastric cancer xenograft model using a daily oral dose of 30 mg\/kg. These results suggest that III is a promising candidate for further drug development.<\/p>\n

European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 1046832-21-6 belongs to class pyrazoles-derivatives, and the molecular formula is C11H19BN2O2, Application of C11H19BN2O2<\/a>.<\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

European Journal of Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 1046832-21-6 belongs to class pyrazoles-derivatives, and the molecular formula is C11H19BN2O2, Application of C11H19BN2O2<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[737,131],"tags":[716],"class_list":["post-10276","post","type-post","status-publish","format-standard","hentry","category-1046832-21-6","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nRan, Kai's team published research in European Journal of Medicinal Chemistry in 2021-08-05 | 1046832-21-6 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Ran, Kai; Zeng, Jun; Wan, Guoquan; He, Xiaojie; Feng, Zhanzhan; Xiang, Wang; Wei, Wei; Hu, Xiang; Wang, Ningyu; Liu, Zhihao; Yu, Luoting published the artcile< Design, synthesis and biological evaluations of a series of Pyrido[1,2-a]pyrimidinone derivatives as novel selective FGFR inhibitors>, Application of C11H19BN2O2, the main research area is pyridopyrimidinone preparation antitumor activity FGFR inhibitor; 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