{"id":11398,"date":"2022-11-25T10:24:26","date_gmt":"2022-11-25T02:24:26","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11398"},"modified":"2022-11-25T10:24:26","modified_gmt":"2022-11-25T02:24:26","slug":"liu-mingmings-team-published-research-in-journal-of-medicinal-chemistry-in-62-cas-763120-58-7","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11398","title":{"rendered":"Liu, Mingming’s team published research in Journal of Medicinal Chemistry in 62 | CAS: 763120-58-7"},"content":{"rendered":"

Liu, Mingming published the artcileDiscovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1\u03b1 Signaling Inhibitors with Potent Activities of Anticancer Metastasis<\/i><\/b>, Computed Properties of 763120-58-7<\/a>, the publication is Journal of Medicinal Chemistry (2019), 62(20), 9299-9314, database is CAplus and MEDLINE.<\/p>\n

In order to discover novel hypoxia-inducible factor 1 (HIF-1) inhibitors for the cancer metastasis treatment, 68 new aryl carboxamide compounds were synthesized and evaluated for their inhibitory effect by dual luciferase-reporter assay. Based on five rounds of investigation on structure-activity relationships step by step, compound I<\/strong> was discovered as the most active inhibitor (IC50<\/sub> = 0.32 \u03bcM) with no obvious cytotoxicity (CC50<\/sub> > 50 \u03bcM). It effectively attenuated hypoxia-induced HIF-1\u03b1 protein accumulation and reduced transcription of vascular epidermal growth factor in a dose-dependent manner, which was further demonstrated by its inhibitory potency on capillary-like tube formation, angiogenesis of zebrafish as well as cellular migration and invasion. Importantly, compound I<\/strong> exhibited antimetastatic potency in breast cancer lung metastasis in the mice model, indicating its promising therapeutic potential for prevention and treatment of tumor metastasis. These results definitely merit attention for further rational design of more efficient HIF-1 inhibitors in the future.<\/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-11398","post","type-post","status-publish","format-standard","hentry","category-763120-58-7","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"\nLiu, Mingming's team published research in Journal of Medicinal Chemistry in 62 | CAS: 763120-58-7 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Liu, Mingming published the artcileDiscovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1\u03b1 Signaling Inhibitors with Potent Activities of Anticancer Metastasis, Computed Properties of 763120-58-7, the publication is Journal of Medicinal Chemistry (2019), 62(20), 9299-9314, 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=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11398\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Liu, Mingming's team published research in Journal of Medicinal Chemistry in 62 | CAS: 763120-58-7 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Liu, Mingming published the artcileDiscovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1\u03b1 Signaling Inhibitors with Potent Activities of Anticancer Metastasis, Computed Properties of 763120-58-7, the publication is Journal of Medicinal Chemistry (2019), 62(20), 9299-9314, database is CAplus and MEDLINE.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11398\" \/>\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\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11398\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11398\",\"name\":\"Liu, Mingming's team published research in Journal of Medicinal Chemistry in 62 | CAS: 763120-58-7 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-11-25T02:24:26+00:00\",\"author\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Liu, Mingming published the artcileDiscovery of Novel Aryl Carboxamide Derivatives as Hypoxia-Inducible Factor 1\u03b1 Signaling Inhibitors with Potent Activities of Anticancer Metastasis, Computed Properties of 763120-58-7, the publication is Journal of Medicinal Chemistry (2019), 62(20), 9299-9314, database is CAplus and MEDLINE.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11398#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=11398\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11398#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"https:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Liu, Mingming’s team published research in Journal of Medicinal Chemistry in 62 | 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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