{"id":12200,"date":"2023-02-09T10:49:41","date_gmt":"2023-02-09T02:49:41","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=12200"},"modified":"2023-02-09T10:49:41","modified_gmt":"2023-02-09T02:49:41","slug":"raffa-demetrio-et-al-published-their-research-in-european-journal-of-medicinal-chemistry-in-2004-cas-3528-58-3","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=12200","title":{"rendered":"Raffa, Demetrio et al. published their research in European Journal of Medicinal Chemistry in 2004 | CAS: 3528-58-3"},"content":{"rendered":"<p>Synthesis, cytotoxicity, and inhibitory effects on tubulin polymerization of a new 3-heterocyclo substituted 2-styrylquinazolinones was written by Raffa, Demetrio;Edler, Michael C.;Daidone, Giuseppe;Maggio, Benedetta;Merickech, Mourad;Plescia, Salvatore;Schillaci, Domenico;Bai, Ruoli;Hamel, Ernest. And the article was included in European Journal of Medicinal Chemistry in 2004.<a href=\"https:\/\/www.ambeed.com\/products\/3528-58-3.html\">Synthetic Route of C5H9N3<\/a> This article mentions the following:<\/p>\n<p>In order to study the influence of 3-substituents on the cytotoxic activity of 2-styrylquinazolinones, a series of 6-chloro-2-styryl-3-(heteroaryl)-4(3H)-quinazolinones, e.g. <strong>I<\/strong>, were synthesized by refluxing equimolar amounts of the corresponding 2-methyl-quinazolinones and benzaldehyde in glacial acetic acid. At 1 \u03bcg ml<sup>-1<\/sup> concentration, almost all the synthesized compounds showed some cytotoxic activity against the L1210 and K562 leukemia cell lines. However, only compound <strong>I<\/strong> inhibited the growth of these cells by over 50%. It was also found to be the only member of the series that inhibited tubulin polymerization, with an IC<sub>50<\/sub> value of 5.8 vs. 3.2 \u03bcM for control drug colchicine. <strong>I<\/strong> was further examined for effects on the growth of human MCF7 breast carcinoma cells and Burkitt lymphoma CA46 cells, which had IC<sub>50<\/sub> values of 0.34 and 1.0 \u03bcM, resp. At 10 \u03bcM, <strong>I<\/strong> induced G2\/M arrest (66%) in Burkitt cells, with a mitotic index of 20%. At 3.4 \u03bcM, it caused disruption of the cellular microtubule system of the MCF7 cells. Both these cellular effects are consistent with its mechanism of action resulting from its inhibitory effect on tubulin assembly. In the experiment, the researchers used many compounds, for example, 1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3<a href=\"https:\/\/www.ambeed.com\/products\/3528-58-3.html\">Synthetic Route of C5H9N3<\/a>).<\/p>\n<p>1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities.<a href=\"https:\/\/www.ambeed.com\/products\/3528-58-3.html\">Synthetic Route of C5H9N3<\/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>1-Ethyl-1H-pyrazol-5-amine (cas: 3528-58-3) belongs to pyrazole derivatives. An alternative way to synthesize multisubstituted pyrazoles is the Csingle bondH arylation of simple pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, antidiabetic and antibacterial activities.<a href=\"https:\/\/www.ambeed.com\/products\/3528-58-3.html\">Synthetic Route of C5H9N3<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[830,131],"tags":[128],"class_list":["post-12200","post","type-post","status-publish","format-standard","hentry","category-3528-58-3","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>Raffa, Demetrio et al. published their research in European Journal of Medicinal Chemistry in 2004 | CAS: 3528-58-3 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Synthesis, cytotoxicity, and inhibitory effects on tubulin polymerization of a new 3-heterocyclo substituted 2-styrylquinazolinones was written by Raffa, Demetrio;Edler, Michael C.;Daidone, Giuseppe;Maggio, Benedetta;Merickech, Mourad;Plescia, Salvatore;Schillaci, Domenico;Bai, Ruoli;Hamel, Ernest. And the article was included in European Journal of Medicinal Chemistry in 2004.Synthetic Route of C5H9N3 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=12200\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Raffa, Demetrio et al. published their research in European Journal of Medicinal Chemistry in 2004 | CAS: 3528-58-3 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Synthesis, cytotoxicity, and inhibitory effects on tubulin polymerization of a new 3-heterocyclo substituted 2-styrylquinazolinones was written by Raffa, Demetrio;Edler, Michael C.;Daidone, Giuseppe;Maggio, Benedetta;Merickech, Mourad;Plescia, Salvatore;Schillaci, Domenico;Bai, Ruoli;Hamel, Ernest. 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And the article was included in European Journal of Medicinal Chemistry in 2004.Synthetic Route of C5H9N3 This article mentions the following:","breadcrumb":{"@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=12200#breadcrumb"},"inLanguage":"en-US","potentialAction":[{"@type":"ReadAction","target":["https:\/\/www.pyrazoles-derivatives.com\/?p=12200"]}]},{"@type":"BreadcrumbList","@id":"https:\/\/www.pyrazoles-derivatives.com\/?p=12200#breadcrumb","itemListElement":[{"@type":"ListItem","position":1,"name":"\u9996\u9875","item":"http:\/\/www.pyrazoles-derivatives.com\/"},{"@type":"ListItem","position":2,"name":"Raffa, Demetrio et al. published their research in European Journal of Medicinal Chemistry in 2004 | CAS: 3528-58-3"}]},{"@type":"WebSite","@id":"http:\/\/www.pyrazoles-derivatives.com\/#website","url":"http:\/\/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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