{"id":11453,"date":"2022-11-25T10:28:57","date_gmt":"2022-11-25T02:28:57","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11453"},"modified":"2022-11-25T10:28:57","modified_gmt":"2022-11-25T02:28:57","slug":"cui-j-jeans-team-published-research-in-journal-of-medicinal-chemistry-in-55-cas-763120-58-7","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11453","title":{"rendered":"Cui, J. Jean’s team published research in Journal of Medicinal Chemistry in 55 | CAS: 763120-58-7"},"content":{"rendered":"

Cui, J. Jean published the artcileDiscovery of a Novel Class of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (c-MET) Protein Kinase Inhibitors and Identification of the Clinical Candidate 2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the Treatment of Cancer<\/i><\/b>, HPLC of Formula: 763120-58-7<\/a>, the publication is Journal of Medicinal Chemistry (2012), 55(18), 8091-8109, database is CAplus and MEDLINE.<\/p>\n

The c-MET receptor tyrosine kinase is an attractive oncol. target because of its critical role in human oncogenesis and tumor progression. An oxindole hydrazide hit 6 (VI<\/strong>) was identified during a c-MET HTS campaign and subsequently demonstrated to have an unusual degree of selectivity against a broad array of other kinases. The cocrystal structure of the related oxindole hydrazide c-MET inhibitor 10 (X<\/strong>) with a nonphosphorylated c-MET kinase domain revealed a unique binding mode associated with the exquisite selectivity profile. The chem. labile oxindole hydrazide scaffold was replaced with a chem. and metabolically stable triazolopyrazine scaffold using structure based drug design. Medicinal chem. lead optimization produced 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (2, II<\/strong>, PF-04217903), an extremely potent and exquisitely selective c-MET inhibitor. 2 Demonstrated effective tumor growth inhibition in c-MET dependent tumor models with good oral PK properties and an acceptable safety profile in preclin. studies. 2 Progressed to clin. evaluation in a Phase I oncol. setting.<\/p>\n

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, HPLC of Formula: 763120-58-7<\/a>.<\/p>\n

Referemce:
https:\/\/en.wikipedia.org\/wiki\/Pyrazole<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

Journal of Medicinal Chemistry published new progress about 763120-58-7. 763120-58-7 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Boronic Acids,Boronic acid and ester, name is 1H-Pyrazole-4-boronic acid, and the molecular formula is C3H5BN2O2, HPLC of Formula: 763120-58-7<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[802,131],"tags":[732],"class_list":["post-11453","post","type-post","status-publish","format-standard","hentry","category-763120-58-7","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"\nCui, J. Jean's team published research in Journal of Medicinal Chemistry in 55 | CAS: 763120-58-7 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Cui, J. 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Jean published the artcileDiscovery of a Novel Class of Exquisitely Selective Mesenchymal-Epithelial Transition Factor (c-MET) Protein Kinase Inhibitors and Identification of the Clinical Candidate 2-(4-(1-(Quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the Treatment of Cancer, HPLC of Formula: 763120-58-7, the publication is Journal of Medicinal Chemistry (2012), 55(18), 8091-8109, database is CAplus and MEDLINE.\" \/>\n<meta property=\"og:url\" content=\"http:\/\/www.pyrazoles-derivatives.com\/?p=11453\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-11-25T02:28:57+00:00\" \/>\n<meta name=\"author\" content=\"Jessica.F\" \/>\n<meta name=\"twitter:card\" content=\"summary_large_image\" \/>\n<meta name=\"twitter:label1\" content=\"Written by\" \/>\n\t<meta name=\"twitter:data1\" content=\"Jessica.F\" \/>\n\t<meta name=\"twitter:label2\" content=\"Est. reading time\" \/>\n\t<meta name=\"twitter:data2\" content=\"1 minute\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=11453\",\"url\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=11453\",\"name\":\"Cui, J. 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