{"id":11851,"date":"2022-12-05T07:32:40","date_gmt":"2022-12-04T23:32:40","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11851"},"modified":"2022-12-05T07:32:40","modified_gmt":"2022-12-04T23:32:40","slug":"sagar-satishs-team-published-research-in-european-journal-of-medicinal-chemistry-in-222-cas-930-36-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11851","title":{"rendered":"Sagar, Satish’s team published research in European Journal of Medicinal Chemistry in 222 | CAS: 930-36-9"},"content":{"rendered":"

Sagar, Satish published the artcileStructure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKK\u03b2 phosphorylation for pancreatic cancer therapy<\/i><\/b>, Application of 1-Methylpyrazole<\/a>, the publication is European Journal of Medicinal Chemistry (2021), 113579, database is CAplus and MEDLINE.<\/p>\n

Genetic models validated Inhibitor of nuclear factor (NF) kappa B kinase beta (IKK\u00ce\u00b2) as a therapeutic target for KRAS mutation associated pancreatic cancer. Phosphorylation of the activation loop serine residues (S177, S181) in IKK\u00ce\u00b2 is a key event that drives tumor necrosis factor (TNF) \u00ce\u00b1 induced NF-\u00ce\u00baB mediated gene expression. Here we conducted structure activity relationship (SAR) study to improve potency and oral bioavailability of a quinoxaline analog 13-197 that was previously reported as a NF\u00ce\u00baB inhibitor for pancreatic cancer therapy. The SAR led to the identification of a novel quinoxaline urea analog 84 that reduced the levels of p-IKK\u00ce\u00b2 in dose- and time-dependent studies. When compared to 13-197, analog 84 was \u00e2\u0088?.5-fold more potent in TNF\u00ce\u00b1-induced NF\u00ce\u00baB inhibition and \u00e2\u0088?-fold more potent in inhibiting pancreatic cancer cell growth. Analog 84 exhibited \u00e2\u0088?.3-fold greater exposure (AUC0-\u00e2\u0088? resulting in \u00e2\u0088?.7-fold increase in oral bioavailability (%F) when compared to 13-197. Importantly, oral administration of 84 by itself and in combination of gemcitabine reduced p-IKK\u00ce\u00b2 levels and inhibited pancreatic tumor growth in a xenograft model.<\/p>\n

European Journal of Medicinal Chemistry published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Application of 1-Methylpyrazole<\/a>.<\/p>\n

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

European Journal of Medicinal Chemistry published new progress about 930-36-9. 930-36-9 belongs to pyrazoles-derivatives, auxiliary class Pyrazole, name is 1-Methylpyrazole, and the molecular formula is C4H6N2, Application of 1-Methylpyrazole<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[245,131],"tags":[784],"class_list":["post-11851","post","type-post","status-publish","format-standard","hentry","category-930-36-9","category-pyrazoles-derivatives","tag-m-w50-100"],"yoast_head":"\nSagar, Satish's team published research in European Journal of Medicinal Chemistry in 222 | CAS: 930-36-9 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Sagar, Satish published the artcileStructure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKK\u03b2 phosphorylation for pancreatic cancer therapy, Application of 1-Methylpyrazole, the publication is European Journal of Medicinal Chemistry (2021), 113579, database is CAplus and MEDLINE.\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11851\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Sagar, Satish's team published research in European Journal of Medicinal Chemistry in 222 | CAS: 930-36-9 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Sagar, Satish published the artcileStructure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKK\u03b2 phosphorylation for pancreatic cancer therapy, Application of 1-Methylpyrazole, the publication is European Journal of Medicinal Chemistry (2021), 113579, database is CAplus and MEDLINE.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11851\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-12-04T23:32:40+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\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11851\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11851\",\"name\":\"Sagar, Satish's team published research in European Journal of Medicinal Chemistry in 222 | CAS: 930-36-9 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-12-04T23:32:40+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Sagar, Satish published the artcileStructure activity relationship (SAR) study identifies a quinoxaline urea analog that modulates IKK\u03b2 phosphorylation for pancreatic cancer therapy, Application of 1-Methylpyrazole, the publication is European Journal of Medicinal Chemistry (2021), 113579, database is CAplus and MEDLINE.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11851#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=11851\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11851#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Sagar, Satish’s team published research in European Journal of Medicinal Chemistry in 222 | CAS: 930-36-9\"}]},{\"@type\":\"WebSite\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/\",\"name\":\"pyrazoles-derivatives\",\"description\":\"Several pyrazole derivatives possess important pharmacological activities and they have been proved useful materials in drug research. 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