{"id":10013,"date":"2022-10-13T03:03:51","date_gmt":"2022-10-12T19:03:51","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10013"},"modified":"2022-10-13T03:03:51","modified_gmt":"2022-10-12T19:03:51","slug":"yu-jiangs-team-published-research-in-biochemical-pharmacology-amsterdam-netherlands-in-2020-cas-847818-74-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10013","title":{"rendered":"Yu, Jiang&#8217;s team published research in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020 | CAS: 847818-74-0"},"content":{"rendered":"<p>\u300aMetabolically stable diphenylamine derivatives suppress androgen receptor and BET protein in prostate cancer\u300b was published in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020. These research results belong to Yu, Jiang; Zhou, Peiting; Du, Wu; Xu, Ruixue; Yan, Guoyi; Deng, Yufang; Li, Xinghai; Chen, Yuanwei. <a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">Recommanded Product: 847818-74-0<\/a> The article mentions the following:<\/p>\n<p>Androgen receptor (AR) is a crucial driver of prostate cancer (PC). AR-relevant resistance remains a major challenge in castration-resistant prostate cancer (CRPC). Bromodomain and extra-terminal domain (BET) family are critical AR coregulators. Here, we developed several diphenylamine derivatives and identified compound 7d that disrupted the functions of AR and BET family in prostate cancer and exhibited favorable metabolic stability in vitro and high drug exposure in vivo. We showed 7d not only bound to AR, suppressed transactivation of wild-type AR (wt-AR) and the mutant that mediates Enzalutamide resistance, but also reduced c-Myc protein expression through BET inhibition. In addition, 7d inhibited the proliferation of AR-pos. PC cells with favorable selectivity and suppressed AR-V7-expressing VCaP and 22Rv1 xenografts growth in vivo. Collectively, these results indicate the potential of lead compound 7d as an orally available AR and BET inhibitor to treat CRPC and overcome antiandrogen resistance. In the experiment, the researchers used many compounds, for example, 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0<a href=\"https:\/\/www.ambeed.com\/products\/847818-74-0.html\">Recommanded Product: 847818-74-0<\/a>)<\/p>\n<p>1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to 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\/847818-74-0.html\">Recommanded Product: 847818-74-0<\/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-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0) belongs to 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\/847818-74-0.html\">Recommanded Product: 847818-74-0<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[744,131],"tags":[129],"class_list":["post-10013","post","type-post","status-publish","format-standard","hentry","category-847818-74-0","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Yu, Jiang&#039;s team published research in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020 | CAS: 847818-74-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"\u300aMetabolically stable diphenylamine derivatives suppress androgen receptor and BET protein in prostate cancer\u300b was published in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020. These research results belong to Yu, Jiang; Zhou, Peiting; Du, Wu; Xu, Ruixue; Yan, Guoyi; Deng, Yufang; Li, Xinghai; Chen, Yuanwei. Recommanded Product: 847818-74-0 The 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=10013\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Yu, Jiang&#039;s team published research in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020 | CAS: 847818-74-0 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"\u300aMetabolically stable diphenylamine derivatives suppress androgen receptor and BET protein in prostate cancer\u300b was published in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020. These research results belong to Yu, Jiang; Zhou, Peiting; Du, Wu; Xu, Ruixue; Yan, Guoyi; Deng, Yufang; Li, Xinghai; Chen, Yuanwei. 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These research results belong to Yu, Jiang; Zhou, Peiting; Du, Wu; Xu, Ruixue; Yan, Guoyi; Deng, Yufang; Li, Xinghai; Chen, Yuanwei. 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These research results belong to Yu, Jiang; Zhou, Peiting; Du, Wu; Xu, Ruixue; Yan, Guoyi; Deng, Yufang; Li, Xinghai; Chen, Yuanwei. Recommanded Product: 847818-74-0 The article mentions the following:","robots":{"index":"index","follow":"follow","max-snippet":"max-snippet:-1","max-image-preview":"max-image-preview:large","max-video-preview":"max-video-preview:-1"},"canonical":"https:\/\/www.pyrazoles-derivatives.com\/?p=10013","og_locale":"en_US","og_type":"article","og_title":"Yu, Jiang's team published research in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020 | CAS: 847818-74-0 | pyrazoles-derivatives","og_description":"\u300aMetabolically stable diphenylamine derivatives suppress androgen receptor and BET protein in prostate cancer\u300b was published in Biochemical Pharmacology (Amsterdam, Netherlands) in 2020. These research results belong to Yu, Jiang; Zhou, Peiting; Du, Wu; Xu, Ruixue; Yan, Guoyi; Deng, Yufang; Li, Xinghai; Chen, Yuanwei. 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