{"id":11400,"date":"2022-11-25T10:24:26","date_gmt":"2022-11-25T02:24:26","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11400"},"modified":"2022-11-25T10:24:26","modified_gmt":"2022-11-25T02:24:26","slug":"tng-jiahuis-team-published-research-in-journal-of-medicinal-chemistry-in-63-cas-724710-02-5","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11400","title":{"rendered":"Tng, Jiahui’s team published research in Journal of Medicinal Chemistry in 63 | CAS: 724710-02-5"},"content":{"rendered":"

Tng, Jiahui published the artcileAchiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation<\/i><\/b>, Name: (1H-Pyrazol-5-yl)boronic acid<\/a>, the publication is Journal of Medicinal Chemistry (2020), 63(11), 5956-5971, database is CAplus and MEDLINE.<\/p>\n

AR-42 is an orally active inhibitor of histone deacetylases (HDACs) in clin. trials for multiple myeloma, leukemia, and lymphoma. It has few hydrogen bond donors and acceptors but is a chiral 2-arylbutyrate and potentially prone to racemization. We report achiral AR-42 analogs incorporating a cycloalkyl group linked via a quaternary carbon atom, with up to 40-fold increased potency against human class I HDACs (e.g., JT86, IC50<\/sub> 0.7 nM, HDAC1), 25-fold increased cytotoxicity against five human cancer cell lines, and up to 70-fold less toxicity in normal human cells. JT86(I<\/strong>) was ninefold more potent than racAR-42 in promoting accumulation of acetylated histone H4 in MM96L melanoma cells. Mol. modeling and structure-activity relationships support binding to HDAC1 with tetrahydropyran acting as a hydrophobic shield from water at the enzyme surface. Such potent inhibitors of class I HDACs may show benefits in diseases (cancers, parasitic infections, inflammatory conditions) where AR-42 is active.<\/p>\n

Journal of Medicinal Chemistry published new progress about 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C22H32O2, Name: (1H-Pyrazol-5-yl)boronic acid<\/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 724710-02-5. 724710-02-5 belongs to pyrazoles-derivatives, auxiliary class Pyrazole,Boronic acid and ester,Pyrazole,Boronic Acids,Boronic acid and ester, name is (1H-Pyrazol-5-yl)boronic acid, and the molecular formula is C22H32O2, Name: (1H-Pyrazol-5-yl)boronic acid<\/a>.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[801,131],"tags":[732],"class_list":["post-11400","post","type-post","status-publish","format-standard","hentry","category-724710-02-5","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"\nTng, Jiahui's team published research in Journal of Medicinal Chemistry in 63 | CAS: 724710-02-5 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Tng, Jiahui published the artcileAchiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation, Name: (1H-Pyrazol-5-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2020), 63(11), 5956-5971, 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=11400\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Tng, Jiahui's team published research in Journal of Medicinal Chemistry in 63 | CAS: 724710-02-5 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Tng, Jiahui published the artcileAchiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation, Name: (1H-Pyrazol-5-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2020), 63(11), 5956-5971, database is CAplus and MEDLINE.\" \/>\n<meta property=\"og:url\" content=\"http:\/\/www.pyrazoles-derivatives.com\/?p=11400\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-11-25T02:24:26+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=11400\",\"url\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=11400\",\"name\":\"Tng, Jiahui's team published research in Journal of Medicinal Chemistry in 63 | CAS: 724710-02-5 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-11-25T02:24:26+00:00\",\"author\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Tng, Jiahui published the artcileAchiral Derivatives of Hydroxamate AR-42 Potently Inhibit Class I HDAC Enzymes and Cancer Cell Proliferation, Name: (1H-Pyrazol-5-yl)boronic acid, the publication is Journal of Medicinal Chemistry (2020), 63(11), 5956-5971, database is CAplus and MEDLINE.\",\"breadcrumb\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=11400#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"http:\/\/www.pyrazoles-derivatives.com\/?p=11400\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/?p=11400#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"http:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Tng, Jiahui’s team published research in Journal of Medicinal Chemistry in 63 | CAS: 724710-02-5\"}]},{\"@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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