{"id":10777,"date":"2022-10-28T06:39:16","date_gmt":"2022-10-27T22:39:16","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10777"},"modified":"2022-10-28T06:39:16","modified_gmt":"2022-10-27T22:39:16","slug":"zhang-lingtian-team-published-research-in-european-journal-of-medicinal-chemistry-in-2021-761446-44-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10777","title":{"rendered":"Zhang, Lingtian team published research in European Journal of Medicinal Chemistry in 2021 | 761446-44-0"},"content":{"rendered":"

Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. Computed Properties of 761446-44-0<\/a>.<\/p>\n

Zhang, Lingtian;Lakkaniga, Naga Rajiv;Bharate, Jaideep B.;Mcconnell, Nicholas;Wang, Xiuqi;Kharbanda, Anupreet;Leung, Yuet-Kin;Frett, Brendan;Shah, Neil P.;Li, Hong-yu research published \u300a Discovery of imidazo[1,2-a]pyridine-thiophene derivatives as FLT3 and FLT3 mutants inhibitors for acute myeloid leukemia through structure-based optimization of an NEK2 inhibitor\u300b, the research content is summarized as follows. FMS-like tyrosine kinase 3 (FLT3) with an internal tandem duplication (ITD) mutation has been validated as a driver lesion and a therapeutic target for acute myeloid leukemia (AML). Currently, several potent small-mol. FLT3 kinase inhibitors are being evaluated or have completed evaluation in clin. trials. However, many of these inhibitors are challenged by the secondary mutations on kinase domain, especially the point mutations at the activation loop (D835) and gatekeeper residue (F691). To overcome the resistance challenge, we identified a novel series of imidazo[1,2-a]pyridine-thiophene derivatives from a NIMA-related kinase 2 (NEK2) kinase inhibitor CMP3a, which retained inhibitory activities on FTL3-ITDD835V and FLT3-ITDF691L. Through this study, we identified the imidazo[1,2-a]pyridine-thiophene derivatives as type-I inhibitors of FLT3. Moreover, we observed compound 5o as an inhibitor displaying equal anti-proliferative activities against FLT3-ITD, FTL3-ITDD835Y and FLT3-ITDF691L driven acute myeloid leukemia (AML) cell lines. Meanwhile, the apoptotic effects of compound supported its mechanism of anti-proliferative action. These results indicate that the imidazo[1,2-a]pyridine-thiophene scaffold is promising for targeting acquired resistance caused by FLT3 secondary mutations and compound 5o is an interesting lead in this direction.<\/p>\n

761446-44-0, 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%., Computed Properties of 761446-44-0<\/a><\/p>\n

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

761446-44-0, 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%., Computed Properties of 761446-44-0<\/a><\/p>\n","protected":false},"author":8,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[733,131],"tags":[716],"class_list":["post-10777","post","type-post","status-publish","format-standard","hentry","category-761446-44-0","category-pyrazoles-derivatives","tag-m-w200-250"],"yoast_head":"\nZhang, Lingtian team published research in European Journal of Medicinal Chemistry in 2021 | 761446-44-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Pyrazole is an organic compound with the formula C3H3N2H. It is a heterocycle characterized by a 5-membered ring of three carbon atoms and two adjacent nitrogen atoms, which are in ortho-substitution. 761446-44-0, formula is C10H17BN2O2, Name is 1-Methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Pyrazoles are a class of compounds that have the ring C3N2 with adjacent nitrogen atoms.Notable drugs containing a pyrazole ring are celecoxib (celebrex) and the anabolic steroid stanozolol. 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