{"id":11789,"date":"2022-12-05T02:37:14","date_gmt":"2022-12-04T18:37:14","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=11789"},"modified":"2022-12-05T02:37:14","modified_gmt":"2022-12-04T18:37:14","slug":"naus-petrs-team-published-research-in-journal-of-medicinal-chemistry-in-53-cas-763120-58-7","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=11789","title":{"rendered":"Naus, Petr’s team published research in Journal of Medicinal Chemistry in 53 | CAS: 763120-58-7"},"content":{"rendered":"

Naus, Petr published the artcile6-(Het)aryl-7-Deazapurine Ribonucleosides as Novel Potent Cytostatic Agents<\/i><\/b>, Safety of 1H-Pyrazole-4-boronic acid<\/a>, the publication is Journal of Medicinal Chemistry (2010), 53(1), 460-470, database is CAplus and MEDLINE.<\/p>\n

A series of novel 7-deazapurine ribonucleosides, e.g. I<\/strong>, bearing an alkyl, aryl, or hetaryl group in position 6 and H, F, or Cl atom in position 7, has been prepared either by Pd-catalyzed cross-coupling reactions of the corresponding protected 6-chloro-(7-halogenated-)7-deazapurine ribonucleosides with alkyl- or (het)arylorganometallics followed by deprotection, or by single-step aqueous phase cross-coupling reactions of unprotected 6-chloro-(7-halogenated-)7-deazapurine ribonucleosides with (het)arylboronic acids. Significant cytostatic effect was detected with a substantial proportion of the prepared compounds The most potent were 7-H or 7-F derivatives of 6-furyl- or 6-thienyl-7-deazapurines displaying cytostatic activity in multiple cancer cell lines with a geometric mean of 50% growth inhibition concentration ranging from 16 to 96 nM, a potency comparable to or better than that of the nucleoside analog clofarabine. Intracellular phosphorylation to mono- and triphosphates and the inhibition of total RNA synthesis was demonstrated in preliminary study of metabolism and mechanism of action studies.<\/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, Safety of 1H-Pyrazole-4-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 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, Safety of 1H-Pyrazole-4-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":[802,131],"tags":[732],"class_list":["post-11789","post","type-post","status-publish","format-standard","hentry","category-763120-58-7","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"\nNaus, Petr's team published research in Journal of Medicinal Chemistry in 53 | CAS: 763120-58-7 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Naus, Petr published the artcile6-(Het)aryl-7-Deazapurine Ribonucleosides as Novel Potent Cytostatic Agents, Safety of 1H-Pyrazole-4-boronic acid, the publication is Journal of Medicinal Chemistry (2010), 53(1), 460-470, 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=11789\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Naus, Petr's team published research in Journal of Medicinal Chemistry in 53 | CAS: 763120-58-7 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Naus, Petr published the artcile6-(Het)aryl-7-Deazapurine Ribonucleosides as Novel Potent Cytostatic Agents, Safety of 1H-Pyrazole-4-boronic acid, the publication is Journal of Medicinal Chemistry (2010), 53(1), 460-470, database is CAplus and MEDLINE.\" \/>\n<meta property=\"og:url\" content=\"https:\/\/www.pyrazoles-derivatives.com\/?p=11789\" \/>\n<meta property=\"og:site_name\" content=\"pyrazoles-derivatives\" \/>\n<meta property=\"article:published_time\" content=\"2022-12-04T18:37:14+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=11789\",\"url\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11789\",\"name\":\"Naus, Petr's team published research in Journal of Medicinal Chemistry in 53 | CAS: 763120-58-7 | pyrazoles-derivatives\",\"isPartOf\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#website\"},\"datePublished\":\"2022-12-04T18:37:14+00:00\",\"author\":{\"@id\":\"http:\/\/www.pyrazoles-derivatives.com\/#\/schema\/person\/d9a9f27bed675392c6f363a01ffd49f1\"},\"description\":\"Naus, Petr published the artcile6-(Het)aryl-7-Deazapurine Ribonucleosides as Novel Potent Cytostatic Agents, Safety of 1H-Pyrazole-4-boronic acid, the publication is Journal of Medicinal Chemistry (2010), 53(1), 460-470, database is CAplus and MEDLINE.\",\"breadcrumb\":{\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11789#breadcrumb\"},\"inLanguage\":\"en-US\",\"potentialAction\":[{\"@type\":\"ReadAction\",\"target\":[\"https:\/\/www.pyrazoles-derivatives.com\/?p=11789\"]}]},{\"@type\":\"BreadcrumbList\",\"@id\":\"https:\/\/www.pyrazoles-derivatives.com\/?p=11789#breadcrumb\",\"itemListElement\":[{\"@type\":\"ListItem\",\"position\":1,\"name\":\"\u9996\u9875\",\"item\":\"http:\/\/www.pyrazoles-derivatives.com\/\"},{\"@type\":\"ListItem\",\"position\":2,\"name\":\"Naus, Petr’s team published research in Journal of Medicinal Chemistry in 53 | CAS: 763120-58-7\"}]},{\"@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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