{"id":11749,"date":"2022-12-02T03:54:23","date_gmt":"2022-12-01T19:54:23","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11749"},"modified":"2022-12-02T03:54:23","modified_gmt":"2022-12-01T19:54:23","slug":"ran-xus-team-published-research-in-journal-of-medicinal-chemistry-in-58-cas-763120-58-7","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11749","title":{"rendered":"Ran, Xu’s team published research in Journal of Medicinal Chemistry in 58 | CAS: 763120-58-7"},"content":{"rendered":"

Ran, Xu published the artcileStructure-Based Design of \u03b3-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors<\/i><\/b>, Computed Properties of 763120-58-7<\/a>, the publication is Journal of Medicinal Chemistry (2015), 58(12), 4927-4939, database is CAplus and MEDLINE.<\/p>\n

Small-mol. inhibitors of bromodomain and extra terminal proteins (BET), including BRD2, BRD3, and BRD4 proteins have therapeutic potential for the treatment of human cancers and other diseases and conditions. In this paper, the authors report the design, synthesis, and evaluation of \u03b3-carboline-containing compounds as a new class of small-mol. BET inhibitors. The most potent inhibitor I<\/strong> (RX-37) obtained from this study binds to BET bromodomain proteins (BRD2, BRD3, and BRD4) with Ki<\/sub> values of 3.2-24.7 nM and demonstrates high selectivity over other non-BET bromodomain-containing proteins. Compound I<\/strong> potently and selectively inhibits cell growth in human acute leukemia cell lines harboring the rearranged mixed lineage leukemia 1 gene. The authors have determined a cocrystal structure of I<\/strong> in complex with BRD4 BD2 at 1.4 \u00c5 resolution, which provides a solid structural basis for the compound’s high binding affinity and for its further structure-based optimization. Compound I<\/strong> represents a promising lead compound for the development of a new class of therapeutics for the treatment of human cancer and other conditions.<\/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, Computed Properties of 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, Computed Properties of 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-11749","post","type-post","status-publish","format-standard","hentry","category-763120-58-7","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"\nRan, Xu's team published research in Journal of Medicinal Chemistry in 58 | CAS: 763120-58-7 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Ran, Xu published the artcileStructure-Based Design of \u03b3-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors, Computed Properties of 763120-58-7, the publication is Journal of Medicinal Chemistry (2015), 58(12), 4927-4939, 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=\"http:\/\/www.pyrazoles-derivatives.com\/?p=11749\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Ran, Xu's team published research in Journal of Medicinal Chemistry in 58 | CAS: 763120-58-7 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Ran, Xu published the artcileStructure-Based Design of \u03b3-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors, Computed Properties of 763120-58-7, the publication is Journal of Medicinal Chemistry (2015), 58(12), 4927-4939, database is CAplus and MEDLINE.\" \/>\n<meta property=\"og:url\" content=\"http:\/\/www.pyrazoles-derivatives.com\/?p=11749\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-12-01T19:54:23+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=11749\",\"url\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=11749\",\"name\":\"Ran, Xu's team published research in Journal of Medicinal Chemistry in 58 | CAS: 763120-58-7 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-12-01T19:54:23+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Ran, Xu published the artcileStructure-Based Design of \u03b3-Carboline Analogues as Potent and Specific BET Bromodomain Inhibitors, Computed Properties of 763120-58-7, the publication is Journal of Medicinal Chemistry (2015), 58(12), 4927-4939, database is CAplus and MEDLINE.\",\"breadcrumb\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=11749#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"http:\/\/www.pyrazoles-derivatives.com\/?p=11749\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=11749#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Ran, Xu’s team published research in Journal of Medicinal Chemistry in 58 | CAS: 763120-58-7\"}]},{\"@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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