{"id":10724,"date":"2022-10-28T06:36:50","date_gmt":"2022-10-27T22:36:50","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10724"},"modified":"2022-10-28T06:36:50","modified_gmt":"2022-10-27T22:36:50","slug":"wang-ruifeng-team-published-research-in-bioorganic-chemistry-in-2020-2075-46-9","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10724","title":{"rendered":"Wang, Ruifeng team published research in Bioorganic Chemistry  in 2020 | 2075-46-9"},"content":{"rendered":"<p>Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is  4-Nitro-1H-pyrazole.  Pyrazole is a weak base, with pKb 11.5 (pKa of the conjugated acid 2.49 at 25 \u00b0C).Pyrazole used as a ligand to prepare organometallic compounds. <a href=\"https:\/\/www.ambeed.com\/products\/2075-46-9.html\">Product Details of C3H3N3O2<\/a>.<\/p>\n<p>Wang, Ruifeng;Zhao, Xiangxin;Yu, Sijia;Chen, Yixuan;Cui, Hengxian;Wu, Tianxiao;Hao, Chenzhou;Zhao, Dongmei;Cheng, Maosheng research published \u300a Discovery of 7H-pyrrolo[2,3-d]pyridine derivatives as potent FAK inhibitors: Design, synthesis, biological evaluation and molecular docking study\u300b, the research content is summarized as follows. Focal adhesion kinase (FAK) is an intracellular non-receptor tyrosine kinase responsible for development of various tumor types. Aiming to explore new potent inhibitors, two series of 2,4-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives were designed and synthesized on the base of structure-based design strategy. Biol. evaluation indicated that most of these new compounds could potently inhibit FAK kinase, leading to the promising inhibitors against the proliferation of U-87MG, A-549, and MDA-MB-231 cancer cell lines. Among them, the optimized compound <strong>I<\/strong> potently inhibited the enzyme (IC<sub>50<\/sub> = 19.1 nM) and displayed stronger potency than TAE-226 in U-87MG, A-549 and MDA-MB-231 cells, with IC<sub>50<\/sub> values of 0.35, 0.24, and 0.34\u03bcM, resp. Compound <strong>I<\/strong> is a multi-target kinase inhibitor. Furthermore, compound <strong>I<\/strong> also exhibited relatively less cytotoxicity (IC<sub>50<\/sub> = 3.72\u03bcM) toward a normal human cell line, HK2. According to the flow cytometry and wound healing assay results, compound <strong>I<\/strong> effectively induced apoptosis and G0\/G1 phase arrest of MDA-MB-231 cells and suppressed the migration of U-87MG, A-549 and MDA-MB-231 cells. The docking study of compound <strong>I<\/strong> was performed to elucidate its possible binding modes and to provide a structural basis for the further structural guidance design of FAK inhibitors. Collectively, these data support the further development of compound <strong>I<\/strong> as a lead compound for FAK-targeted anticancer drug discovery.<\/p>\n<p><a href=\"https:\/\/www.ambeed.com\/products\/2075-46-9.html\">Product Details of C3H3N3O2<\/a>, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g\/mol. The purity is usually 95%.<\/p>\n<p>4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson&#8217;s disease., 2075-46-9.<\/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><a href=\"https:\/\/www.ambeed.com\/products\/2075-46-9.html\">Product Details of C3H3N3O2<\/a>, 4-Nitro-1H-pyrazole, also known as 4-Nitropyrazole, is a useful research compound. Its molecular formula is C3H3N3O2 and its molecular weight is 113.08 g\/mol. The purity is usually 95%.<\/p>\n<p>4-Nitropyrazole, is a building block for the synthesis of various pharmaceutical compounds, including inhibitors, and therapeutic agents. It can be used for the synthesis of highly selective, brain-penetrant aminopyrazole LRRK2 Inhibitor, as a potentially viable treatment for Parkinson&#8217;s disease., 2075-46-9.<\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[152,131],"tags":[732],"class_list":["post-10724","post","type-post","status-publish","format-standard","hentry","category-2075-46-9","category-pyrazoles-derivatives","tag-m-w100-150"],"yoast_head":"<!-- This site is optimized with the Yoast SEO plugin v24.9 - https:\/\/yoast.com\/wordpress\/plugins\/seo\/ -->\n<title>Wang, Ruifeng team published research in Bioorganic Chemistry in 2020 | 2075-46-9 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. 2075-46-9, formula is C3H3N3O2, Name is 4-Nitro-1H-pyrazole. 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