{"id":11873,"date":"2022-12-30T07:41:31","date_gmt":"2022-12-29T23:41:31","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11873"},"modified":"2022-12-30T07:41:31","modified_gmt":"2022-12-29T23:41:31","slug":"yasuda-yorinobu-et-al-published-their-research-in-bioorganic-medicinal-chemistry-in-2015-cas-15953-73-8","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11873","title":{"rendered":"Yasuda, Yorinobu et al. published their research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 15953-73-8"},"content":{"rendered":"<p>Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors was written by Yasuda, Yorinobu;Arakawa, Takeaki;Nawata, Yumi;Shimada, Sayaka;Oishi, Shinya;Fujii, Nobutaka;Nishimura, Shinichi;Hattori, Akira;Kakeya, Hideaki. And the article was included in Bioorganic &amp; Medicinal Chemistry in 2015.<a href=\"https:\/\/www.ambeed.com\/products\/15953-73-8.html\">Category: pyrazoles-derivatives<\/a> This article mentions the following:<\/p>\n<p>Hypoxia-inducible factor (HIF)-1 is well known as a promising target for cancer chemotherapy. By screening an inhouse chem. library using a hypoxia-responsive luciferase reporter gene assay, the authors identified CLB-016 containing 1-ethylpyrazole-3-carboxamide as a HIF-1 inhibitor (IC<sub>50<\/sub> = 19.1 \u03bcM). In a subsequent extensive structure-activity relationship (SAR) study, the authors developed compound 11Ae (4-[5-[(4-bromo-3,5-dimethyl-1H-pyrazol-1-yl)methyl]furan-2-carboxamido]-1-ethyl-1H-pyrazole-3-carboxamide) with an IC<sub>50<\/sub> value of 8.1 \u03bcM against HIF-1-driven luciferase activity. CLB-016 and compound 11Ae were shown to significantly suppress the HIF-1-mediated hypoxia response, including carbonic anhydrase IX (CAIX) gene expression and migration of human sarcoma HT1080 cells. These results revealed 1-ethylpyrazole-3-carboxamide as a novel scaffold to develop promising anti-cancer drugs targeting the HIF-1 signaling pathway. In the experiment, the researchers used many compounds, for example, 4-Chloro-3,5-dimethyl-1H-pyrazole (cas: 15953-73-8<a href=\"https:\/\/www.ambeed.com\/products\/15953-73-8.html\">Category: pyrazoles-derivatives<\/a>).<\/p>\n<p>4-Chloro-3,5-dimethyl-1H-pyrazole (cas: 15953-73-8) belongs to pyrazole derivatives. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 \u00b0C).Pyrazole used as a ligand to prepare organometallic compounds. The presence of both electronegative nitrogen atoms in the pyrazole ring reduces the electron density of the C3- and C5-positions leaving electron density of C4-position unaltered. Thus the C4-position is vulnerable to electrophilic attack. The C3 electrophilic-position may undergo deprotonation in the presence of a strong base leading to ring opening.<a href=\"https:\/\/www.ambeed.com\/products\/15953-73-8.html\">Category: pyrazoles-derivatives<\/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-Chloro-3,5-dimethyl-1H-pyrazole (cas: 15953-73-8) belongs to pyrazole derivatives. Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 \u00b0C).Pyrazole used as a ligand to prepare organometallic compounds. The presence of both electronegative nitrogen atoms in the pyrazole ring reduces the electron density of the C3- and C5-positions leaving electron density of C4-position unaltered. Thus the C4-position is vulnerable to electrophilic attack. The C3 electrophilic-position may undergo deprotonation in the presence of a strong base leading to ring opening.<a href=\"https:\/\/www.ambeed.com\/products\/15953-73-8.html\">Category: pyrazoles-derivatives<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[131],"tags":[128],"class_list":["post-11873","post","type-post","status-publish","format-standard","hentry","category-pyrazoles-derivatives","tag-100-200"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Yasuda, Yorinobu et al. published their research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 15953-73-8 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors was written by Yasuda, Yorinobu;Arakawa, Takeaki;Nawata, Yumi;Shimada, Sayaka;Oishi, Shinya;Fujii, Nobutaka;Nishimura, Shinichi;Hattori, Akira;Kakeya, Hideaki. And the article was included in Bioorganic &amp; Medicinal Chemistry in 2015.Category: pyrazoles-derivatives This article mentions the following:\" \/>\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=11873\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Yasuda, Yorinobu et al. published their research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 15953-73-8 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors was written by Yasuda, Yorinobu;Arakawa, Takeaki;Nawata, Yumi;Shimada, Sayaka;Oishi, Shinya;Fujii, Nobutaka;Nishimura, Shinichi;Hattori, Akira;Kakeya, Hideaki. And the article was included in Bioorganic &amp; Medicinal Chemistry in 2015.Category: pyrazoles-derivatives This article mentions the following:\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11873\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-12-29T23:41:31+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=11873\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11873\",\"name\":\"Yasuda, Yorinobu et al. published their research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 15953-73-8 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-12-29T23:41:31+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors was written by Yasuda, Yorinobu;Arakawa, Takeaki;Nawata, Yumi;Shimada, Sayaka;Oishi, Shinya;Fujii, Nobutaka;Nishimura, Shinichi;Hattori, Akira;Kakeya, Hideaki. And the article was included in Bioorganic &amp; Medicinal Chemistry in 2015.Category: pyrazoles-derivatives This article mentions the following:\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11873#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=11873\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11873#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Yasuda, Yorinobu et al. published their research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 15953-73-8\"}]},{\"@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. Pyrazole derivatives play an important role in antitumor agents.\",\"potentialAction\":[{\"@type\":\"SearchAction\",\"target\":{\"@type\":\"EntryPoint\",\"urlTemplate\":\"https:\/\/www.pyrazoles-derivatives.com\/?s={search_term_string}\"},\"query-input\":{\"@type\":\"PropertyValueSpecification\",\"valueRequired\":true,\"valueName\":\"search_term_string\"}}],\"inLanguage\":\"en-US\"},{\"@type\":\"Person\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\",\"name\":\"Jessica.F\",\"image\":{\"@type\":\"ImageObject\",\"inLanguage\":\"en-US\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/image\/\",\"url\":\"https:\/\/weavatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g\",\"contentUrl\":\"https:\/\/weavatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g\",\"caption\":\"Jessica.F\"}}]}<\/script>\n<!-- \/ Yoast SEO plugin. -->","yoast_head_json":{"title":"Yasuda, Yorinobu et al. published their research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 15953-73-8 | pyrazoles-derivatives","description":"Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors was written by Yasuda, Yorinobu;Arakawa, Takeaki;Nawata, Yumi;Shimada, Sayaka;Oishi, Shinya;Fujii, Nobutaka;Nishimura, Shinichi;Hattori, Akira;Kakeya, Hideaki. And the article was included in Bioorganic &amp; Medicinal Chemistry in 2015.Category: pyrazoles-derivatives This article mentions the following:","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":"https:\/\/www.pyrazoles-derivatives.com\/?p=11873","og_locale":"en_US","og_type":"article","og_title":"Yasuda, Yorinobu et al. published their research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 15953-73-8 | pyrazoles-derivatives","og_description":"Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors was written by Yasuda, Yorinobu;Arakawa, Takeaki;Nawata, Yumi;Shimada, Sayaka;Oishi, Shinya;Fujii, Nobutaka;Nishimura, Shinichi;Hattori, Akira;Kakeya, Hideaki. And the article was included in Bioorganic &amp; Medicinal Chemistry in 2015.Category: pyrazoles-derivatives This article mentions the following:","og_url":"https:\/\/www.pyrazoles-derivatives.com\/?p=11873","og_site_name":"pyrazoles-derivatives","article_published_time":"2022-12-29T23:41:31+00:00","author":"Jessica.F","twitter_card":"summary_large_image","twitter_misc":{"Written by":"Jessica.F","Est. reading time":"1 minute"},"schema":{"@context":"https:\/\/schema.org","@graph":[{"@type":"WebPage","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11873","url":"https:\/\/www.pyrazoles-derivatives.com\/?p=11873","name":"Yasuda, Yorinobu et al. published their research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 15953-73-8 | pyrazoles-derivatives","isPartOf":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#website"},"datePublished":"2022-12-29T23:41:31+00:00","author":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1"},"description":"Design, synthesis, and structure-activity relationships of 1-ethylpyrazole-3-carboxamide compounds as novel hypoxia-inducible factor (HIF)-1 inhibitors was written by Yasuda, Yorinobu;Arakawa, Takeaki;Nawata, Yumi;Shimada, Sayaka;Oishi, Shinya;Fujii, Nobutaka;Nishimura, Shinichi;Hattori, Akira;Kakeya, Hideaki. And the article was included in Bioorganic &amp; Medicinal Chemistry in 2015.Category: pyrazoles-derivatives This article mentions the following:","breadcrumb":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11873#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["https:\/\/www.pyrazoles-derivatives.com\/?p=11873"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=11873#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"\u9996\u9875","item":"https:\/\/www.pyrazoles-derivatives.com\/"},{"@type":"ListItem","position":2,"name":"Yasuda, Yorinobu et al. published their research in Bioorganic &amp; Medicinal Chemistry in 2015 | CAS: 15953-73-8"}]},{"@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. Pyrazole derivatives play an important role in antitumor agents.","potentialAction":[{"@type":"SearchAction","target":{"@type":"EntryPoint","urlTemplate":"https:\/\/www.pyrazoles-derivatives.com\/?s={search_term_string}"},"query-input":{"@type":"PropertyValueSpecification","valueRequired":true,"valueName":"search_term_string"}}],"inLanguage":"en-US"},{"@type":"Person","@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1","name":"Jessica.F","image":{"@type":"ImageObject","inLanguage":"en-US","@id":"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/image\/","url":"https:\/\/weavatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g","contentUrl":"https:\/\/weavatar.com\/avatar\/2d1cec2a99eeaad5a5b217c9cdbfb610?s=96&d=mm&r=g","caption":"Jessica.F"}}]}},"_links":{"self":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts\/11873","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/users\/8"}],"replies":[{"embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=11873"}],"version-history":[{"count":0,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=\/wp\/v2\/posts\/11873\/revisions"}],"wp:attachment":[{"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=11873"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=11873"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/www.pyrazoles-derivatives.com\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=11873"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}