{"id":10757,"date":"2022-10-28T06:38:05","date_gmt":"2022-10-27T22:38:05","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10757"},"modified":"2022-10-28T06:38:05","modified_gmt":"2022-10-27T22:38:05","slug":"yang-yaxi-team-published-research-in-journal-of-medicinal-chemistry-in-2020-761446-44-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10757","title":{"rendered":"Yang, Yaxi team published research in Journal of Medicinal Chemistry in 2020 | 761446-44-0"},"content":{"rendered":"

Pyrazoles are synthesized by the reaction of \u03b1,\u03b2-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Related Products of 761446-44-0<\/a>.<\/p>\n

Yang, Yaxi;Zhang, Rukang;Li, Zhaojun;Mei, Lianghe;Wan, Shili;Ding, Hong;Chen, Zhifeng;Xing, Jing;Feng, Huijin;Han, Jie;Jiang, Hualiang;Zheng, Mingyue;Luo, Cheng;Zhou, Bing research published \u300a Discovery of Highly Potent, Selective, and Orally Efficacious p300\/CBP Histone Acetyltransferases Inhibitors\u300b, the research content is summarized as follows. P300 and CREB-binding protein (CBP) are ubiquitously expressed pleiotropic lysine acetyltransferases and play a key role as transcriptional co-activators that are essential for a multitude of cellular processes. Despite great importance, there is a lack of highly selective, potent, druglike p300\/CBP inhibitors. Through the artificial-intelligence-assisted drug discovery pipeline and further optimization, we reported the discovery of novel, highly selective, potent small-mol. inhibitors of p300\/CBP histone acetyltransferases (HAT) with desired druglike properties, exemplified by B026. Our data demonstrated that B026, with half maximal inhibitory concentration (IC50<\/sub>) values of 1.8 nM to p300 and 9.5 nM to CBP enzyme inhibitory activity, is the most potent, selective p300\/CBP HAT inhibitor. Moreover, B026 achieves significant and dose-dependent tumor growth inhibition in an animal model of human cancer, suggesting that B026 is a highly promising p300\/CBP HAT inhibitor and warrants extensive preclin. investigation as a potential clin. development candidate.<\/p>\n

Related Products of 761446-44-0<\/a>, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g\/mol. The purity is usually 95%., 761446-44-0.<\/p>\n

Referemce:
Pyrazole – Wikipedia<\/a>,
Pyrazoles – an overview | ScienceDirect Topics<\/a><\/p>\n","protected":false},"excerpt":{"rendered":"

Related Products of 761446-44-0<\/a>, 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole is a useful research compound. Its molecular formula is C10H17BN2O2 and its molecular weight is 208.07 g\/mol. The purity is usually 95%., 761446-44-0.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[733,131],"tags":[716],"class_list":["post-10757","post","type-post","status-publish","format-standard","hentry","category-761446-44-0","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nYang, Yaxi team published research in Journal of Medicinal Chemistry in 2020 | 761446-44-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Pyrazoles are synthesized by the reaction of \u03b1,\u03b2-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). For example, acetylacetone and hydrazine gives 3,5-dimethylpyrazole. Related Products of 761446-44-0.\" \/>\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=10757\" \/>\n<meta property=\"og:locale\" content=\"en_US\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Yang, Yaxi team published research in Journal of Medicinal Chemistry in 2020 | 761446-44-0 | pyrazoles-derivatives\" \/>\n<meta property=\"og:description\" content=\"Pyrazoles are synthesized by the reaction of \u03b1,\u03b2-unsaturated aldehydes with hydrazine and subsequent dehydrogenation. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Substituted pyrazoles are prepared by condensation of 1,3-diketones with hydrazine (Knorr-type reactions). 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