{"id":10091,"date":"2022-10-14T07:44:21","date_gmt":"2022-10-13T23:44:21","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10091"},"modified":"2022-10-14T07:44:21","modified_gmt":"2022-10-13T23:44:21","slug":"sun-lingyis-team-published-research-in-european-journal-of-medicinal-chemistry-in-2013-cas-1015845-73-4","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10091","title":{"rendered":"Sun, Lingyi&#8217;s team published research in European Journal of Medicinal Chemistry in 2013 | CAS: 1015845-73-4"},"content":{"rendered":"<p>Sun, Lingyi; Bera, Hriday; Chui, Wai Keung published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aSynthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase\u300b.<a href=\"https:\/\/www.ambeed.com\/products\/1015845-73-4.html\">Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine<\/a> The author mentioned the following in the article:<\/p>\n<p>Thymidine phosphorylase (TP) is an enzyme that promotes tumor growth and metastasis and therefore is an attractive druggable target. Using a reported TP inhibitor, 7-deazaxanthine (7DX), as the lead compound; this study was set up to evaluate whether pyrazolo[1,5-a][1,3,5]triazin-2,4-diones and pyrazolo[1,5-a][1,3,5]triazin-2-thioxo-4-ones would exhibit TP inhibitory activity. The pyrazolo[1,5-a][1,3,5]triazine nucleus was constructed using a reaction that annulated the 1,3,5-triazine ring onto a pyrazole scaffold. Among the 52 compounds synthesized and tested, it was found that 1,3-dihydro-pyrazolo[1,5-a][1,3,5]triazin-2-thioxo-4-ones exhibited various extent of inhibitory activity against TP. The best compound I, which bears a para-substituted pentafluorosulfur group, showed an IC50 value of 0.04 \u03bcM, which was around 800 times more potent than the 7DX (IC50 = 32 \u03bcM) under the same bioassay conditions. The results of the study suggested that a substituent with +\u03c3 and +\u03c0 properties inserted at position 4 of a Ph ring that is attached to position 8 of the pyrazolo[1,5-a][1,3,5]triazin-2-thioxo-4-one scaffold would give excellent TP inhibitory action. In addition, I was found to be a non-competitive inhibitor thus suggested that it might interact with TP at a position different from the substrate binding site. In the experimental materials used by the author, we found 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine(cas: 1015845-73-4<a href=\"https:\/\/www.ambeed.com\/products\/1015845-73-4.html\">Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine<\/a>)<\/p>\n<p>4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine(cas: 1015845-73-4) belongs to anime. Amines characteristically form\u00a0salts\u00a0with acids; a\u00a0hydrogen ion, H+, adds to the\u00a0nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral\u00a0electrophiles\u00a0(compounds attracted to regions of negative charge) also react with amines; alkyl halides (R\u2032X) and\u00a0analogous\u00a0alkylating agents are important examples of electrophilic reagents.<a href=\"https:\/\/www.ambeed.com\/products\/1015845-73-4.html\">Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine<\/a><\/p>\n<p>Referemce:<br \/><a href=\"https:\/\/en.wikipedia.org\/wiki\/Pyrazole\">Pyrazole &#8211; Wikipedia<\/a>,<br \/><a href=\"https:\/\/www.sciencedirect.com\/topics\/chemistry\/pyrazoles\">Pyrazoles &#8211; an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"<p>4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine(cas: 1015845-73-4) belongs to anime. Amines characteristically form\u00a0salts\u00a0with acids; a\u00a0hydrogen ion, H+, adds to the\u00a0nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral\u00a0electrophiles\u00a0(compounds attracted to regions of negative charge) also react with amines; alkyl halides (R\u2032X) and\u00a0analogous\u00a0alkylating agents are important examples of electrophilic reagents.<a href=\"https:\/\/www.ambeed.com\/products\/1015845-73-4.html\">Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[308,131],"tags":[129],"class_list":["post-10091","post","type-post","status-publish","format-standard","hentry","category-1015845-73-4","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Sun, Lingyi&#039;s team published research in European Journal of Medicinal Chemistry in 2013 | CAS: 1015845-73-4 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Sun, Lingyi; Bera, Hriday; Chui, Wai Keung published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aSynthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase\u300b.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine The author mentioned the following in the article:\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"http:\/\/www.pyrazoles-derivatives.com\/?p=10091\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Sun, Lingyi&#039;s team published research in European Journal of Medicinal Chemistry in 2013 | CAS: 1015845-73-4 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Sun, Lingyi; Bera, Hriday; Chui, Wai Keung published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aSynthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase\u300b.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine The author mentioned the following in the article:\" \/>\n<meta property=\"og:url\" content=\"http:\/\/www.pyrazoles-derivatives.com\/?p=10091\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-10-13T23:44:21+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=\"2 minutes\" \/>\n<script type=\"application\/ld+json\" class=\"yoast-schema-graph\">{\"@context\":\"https:\/\/schema.org\",\"@graph\":[{\"@type\":\"WebPage\",\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=10091\",\"url\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=10091\",\"name\":\"Sun, Lingyi's team published research in European Journal of Medicinal Chemistry in 2013 | CAS: 1015845-73-4 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-10-13T23:44:21+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Sun, Lingyi; Bera, Hriday; Chui, Wai Keung published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aSynthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase\u300b.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine The author mentioned the following in the article:\",\"breadcrumb\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=10091#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"http:\/\/www.pyrazoles-derivatives.com\/?p=10091\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=10091#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Sun, Lingyi&#8217;s team published research in European Journal of Medicinal Chemistry in 2013 | CAS: 1015845-73-4\"}]},{\"@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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The title of the article was \u300aSynthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase\u300b.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine The author mentioned the following in the article:","robots":{"index":"index","follow":"follow","max-snippet":"max-snippet:-1","max-image-preview":"max-image-preview:large","max-video-preview":"max-video-preview:-1"},"canonical":"http:\/\/www.pyrazoles-derivatives.com\/?p=10091","og_locale":"en_US","og_type":"article","og_title":"Sun, Lingyi's team published research in European Journal of Medicinal Chemistry in 2013 | CAS: 1015845-73-4 | pyrazoles-derivatives","og_description":"Sun, Lingyi; Bera, Hriday; Chui, Wai Keung published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aSynthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase\u300b.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine The author mentioned the following in the article:","og_url":"http:\/\/www.pyrazoles-derivatives.com\/?p=10091","og_site_name":"pyrazoles-derivatives","article_published_time":"2022-10-13T23:44:21+00:00","author":"Jessica.F","twitter_card":"summary_large_image","twitter_misc":{"Written by":"Jessica.F","Est. reading time":"2 minutes"},"schema":{"@context":"https:\/\/schema.org","@graph":[{"@type":"WebPage","@id":"http:\/\/www.pyrazoles-derivatives.com\/?p=10091","url":"http:\/\/www.pyrazoles-derivatives.com\/?p=10091","name":"Sun, Lingyi's team published research in European Journal of Medicinal Chemistry in 2013 | CAS: 1015845-73-4 | pyrazoles-derivatives","isPartOf":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#website"},"datePublished":"2022-10-13T23:44:21+00:00","author":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1"},"description":"Sun, Lingyi; Bera, Hriday; Chui, Wai Keung published an article in European Journal of Medicinal Chemistry. The title of the article was \u300aSynthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase\u300b.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine The author mentioned the following in the article:","breadcrumb":{"@id":"http:\/\/www.pyrazoles-derivatives.com\/?p=10091#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["http:\/\/www.pyrazoles-derivatives.com\/?p=10091"]}]},{"@type":"BreadcrumbList","@id":"http:\/\/www.pyrazoles-derivatives.com\/?p=10091#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"\u9996\u9875","item":"https:\/\/www.pyrazoles-derivatives.com\/"},{"@type":"ListItem","position":2,"name":"Sun, Lingyi&#8217;s team published research in European Journal of Medicinal Chemistry in 2013 | CAS: 1015845-73-4"}]},{"@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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