{"id":10200,"date":"2022-10-17T09:12:10","date_gmt":"2022-10-17T01:12:10","guid":{"rendered":"https:\/\/www.pyrazoles-derivatives.com\/?p=10200"},"modified":"2022-10-17T09:12:10","modified_gmt":"2022-10-17T01:12:10","slug":"luecking-ulrichs-team-published-research-in-journal-of-medicinal-chemistry-in-2020-cas-847818-74-0","status":"publish","type":"post","link":"https:\/\/www.pyrazoles-derivatives.com\/?p=10200","title":{"rendered":"Luecking, Ulrich’s team published research in Journal of Medicinal Chemistry in 2020 | CAS: 847818-74-0"},"content":{"rendered":"

Application In Synthesis of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a>In 2020 ,\u300aDamage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models\u300b was published in Journal of Medicinal Chemistry. The article was written by Luecking, Ulrich; Wortmann, Lars; Wengner, Antje M.; Lefranc, Julien; Lienau, Philip; Briem, Hans; Siemeister, Gerhard; Boemer, Ulf; Denner, Karsten; Schaefer, Martina; Koppitz, Marcus; Eis, Knut; Bartels, Florian; Bader, Benjamin; Bone, Wilhelm; Moosmayer, Dieter; Holton, Simon J.; Eberspaecher, Uwe; Grudzinska-Goebel, Joanna; Schatz, Christoph; Deeg, Gesa; Mumberg, Dominik; von Nussbaum, Franz. The article contains the following contents:<\/p>\n

The ATR kinase plays a key role in the DNA damage response by activating essential signaling pathways of DNA damage repair, especially in response to replication stress. Because DNA damage and replication stress are major sources of genomic instability, selective ATR inhibition has been recognized as a promising new approach in cancer therapy. We now report the identification and preclin. evaluation of the novel, clin. ATR inhibitor BAY 1895344(I). Starting from quinoline 2 with weak ATR inhibitory activity, lead optimization efforts focusing on potency, selectivity, and oral bioavailability led to the discovery of the potent, highly selective, orally available ATR inhibitor BAY 1895344, which exhibited strong monotherapy efficacy in cancer xenograft models that carry certain DNA damage repair deficiencies. Moreover, combination treatment of BAY 1895344 with certain DNA damage inducing chemotherapy resulted in synergistic antitumor activity. BAY 1895344 is currently under clin. investigation in patients with advanced solid tumors and lymphomas (NCT03188965). In the experiment, the researchers used 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 847818-74-0Application In Synthesis of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a>)<\/p>\n

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, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Application In Synthesis of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/a><\/p>\n

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

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, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Application In Synthesis of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole<\/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-10200","post","type-post","status-publish","format-standard","hentry","category-847818-74-0","category-pyrazoles-derivatives","tag-200-300"],"yoast_head":"\nLuecking, Ulrich's team published research in Journal of Medicinal Chemistry in 2020 | CAS: 847818-74-0 | pyrazoles-derivatives<\/title>\n<meta name=\"description\" content=\"Application In Synthesis of 1-Methyl-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazoleIn 2020 ,\u300aDamage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models\u300b was published in Journal of Medicinal Chemistry. The article was written by Luecking, Ulrich; Wortmann, Lars; Wengner, Antje M.; Lefranc, Julien; Lienau, Philip; Briem, Hans; Siemeister, Gerhard; Boemer, Ulf; Denner, Karsten; Schaefer, Martina; Koppitz, Marcus; Eis, Knut; Bartels, Florian; Bader, Benjamin; Bone, Wilhelm; Moosmayer, Dieter; Holton, Simon J.; Eberspaecher, Uwe; Grudzinska-Goebel, Joanna; Schatz, Christoph; Deeg, Gesa; Mumberg, Dominik; von Nussbaum, Franz. 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